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Drug resistance against antimalarials is rendering them increasingly ineffective and so there is a need for the development of new antimalarials. To discover new antimalarial chemotypes a phenotypic screen of the Janssen Jumpstarter library against the P. falciparum asexual stage was undertaken, uncovering the cyclopropyl carboxamide structural hit class. Structure-activity analysis revealed that each structural moiety was largely resistant to change, although small changes led to the frontrunner compound, WJM280, which has potent asexual stage activity (EC50 40 nM) and no human cell cytotoxicity. Forward genetics uncovered that cyclopropyl carboxamide resistant parasites have mutations and an amplification in the cytochrome b gene. Cytochrome b was then verified as the target with profiling against cytochrome b drug-resistant parasites and a mitochondrial oxygen consumption assay. Accordingly, the cyclopropyl carboxamide class was shown to have slow-acting asexual stage activity and activity against male gametes and exoerythrocytic forms. Enhancing metabolic stability to attain efficacy in malaria mouse models remains a challenge in the future development of this antimalarial chemotype.

The document from Chemical Communications, published in 2025, provides a comprehensive list of articles covering various topics in chemistry. The issue includes reviews, feature articles, and communications on subjects such as organic synthesis, materials innovation, and electrochemistry. The journal aims to connect the global chemistry community through impactful publications and interdisciplinary research. [Extracted from the article]

Carboranes are a type of molecular clusters consisting of carbon, hydrogen, and boron atoms. They possess unique characteristics, such as three-dimensional aromaticity, icosahedral geometry, and robustness. Functionalized carboranes have been utilized in various fields, including medicine, materials, and organometallic/coordination chemistry. In this context, selective functionalization of o -carboranes has received tremendous attention, specifically in the regio- and enantioselective modification of the ten chemically similar BH vertices within the carborane cage. In recent years, significant progress has been made in catalytic vertex-specific BH functionalization, as well as achieving enantioselective functionalization of the cage BH. This review provides an overview of the recent advancements in this research field. 1 Introduction 2 Carboxy-Assisted BH Functionalization 2.1 Formation of B–C Bonds 2.2 Formation of B–N Bonds 2.3 Formation of B–O Bonds 2.4 Formation of B–X Bonds 2.5 Consecutive Formation of B–C and B–Y (Y = N, O) Bonds 3 N-Based Directing-Group-Assisted B–H Functionalization 3.1 Acylamino as a Directing Group 3.2 Amide as a Directing Group 3.3 Pyridyl as a Directing Group 3.4 Imine as a Directing Group 4 Phosphinyl-Assisted Cage B–H Functionalization 5 Bidentate-Directing-Group-Assisted B–H Functionalization 6 Other Directing-Group-Assisted B–H Functionalization 7 Conclusions [ABSTRACT FROM AUTHOR]

Polyamides (PAs) represent a class of polymers conducive to chemical recycling, where the amide group acts as a reactive site for degradation agents. However, the inherent stability of the amide group means that chemical recycling of PAs often necessitates stringent conditions, such as high temperatures and pressures, significantly hindering advancements in PA chemical recycling. Moreover, the effectiveness of chemically recycling polyamides into monomers or oligomers—essential components for subsequent polymer synthesis—has not been conclusively verified through comprehensive research. Here, we present the first demonstration of a method for the upcycling of PA6 into high-performance PA derivatives. In the proposed method, PA6 is first degraded into oligomers with reactive end groups via glycolysis, with the reactivity of the resulting glycolysates subsequently verified. This oligomer acts as an intermediate in thermoplastic polyamide elastomer (TPAE) synthesis, facilitating direct integration with flexible polyethylene glycol oligomers into TPAE without requiring further degradation to monomers. The mechanical properties of the resultant TPAEs are commensurate with those previously reported for PA6-based TPAEs. By fine-tuning the reaction time and catalyst concentration, it is possible to control the molecular weight of the PA6 glycolysates, thus adjusting the TPAE's mechanical properties. This study presents an innovative approach that seamlessly combines the degradation process of PA6 with the synthesis pathway of TPAE, thus achieving the cost-effective upcycling of PA6 into TPAE. [ABSTRACT FROM AUTHOR]

N -(Difluoropropenyl)amides/amines are an important class of fluorinated compounds. Here, we report an efficient method for synthesizing these compounds without the use of transition metals. Under simple base-promoted conditions, 3-bromo-3,3-difluoroprop-1-ene reacts with N -methylanilines or N -arylacrylamides, with the elimination of one molecule of HBr, to give the target compound. Another efficient method for synthesizing difluoroalkenes is the reaction of 2-bromo-3,3,3-trifluoroprop-1-ene with indole or its analogues. [ABSTRACT FROM AUTHOR]

Herein, we described an atom-economical and sustainable electrochemically driven triarylamine-catalyzed dehydrogenative phosphorylation coupling of glycine derivatives with phosphine oxides, affording the corresponding phosphorus-containing products in moderate to excellent yields. This green protocol employing recyclable triarylamine as a redox mediator was found to offer excellent atom economy and low E-factor scores. The reaction could be conducted in an undivided cell under mild conditions without the use of metal catalysts or stoichiometric oxidants. The substrate scope was wide, encompassing functionalized glycine esters, amides and peptides bearing various functional groups. Mechanism investigation suggested that triarylamine played a crucial role as a redox mediator in the reaction, and a plausible reaction mechanism was proposed. Notably, scale-up reactions and modifications of drugs and peptides demonstrate the potential of this green and sustainable approach for applications in drug discovery. [ABSTRACT FROM AUTHOR]

Herein, we report an efficient strategy for the synthesis of C4-functionalized novel Pfitzinger acid derivatives via C(sp3)–H bond functionalization. This approach capitalizes on the use of a deep eutectic solvent (DES) comprising N,N′-dimethyl urea and L -(+)-tartaric acid (3 : 1 ratio) at 80 °C as the reaction medium. The 1,2,3,4-tetrahydroacridine-based Pfitzinger acid and its derivatives (methyl/benzyl esters, amides, and Weinreb amides) were used for C4 functionalization with aromatic aldehydes. All the synthesized compounds were evaluated for their dual cholinesterase and α-glucosidase inhibitory activity. Most of the evaluated products showed significant inhibitory activity against AChE, BChE and α-glucosidase enzymes in comparison with standard drug tacrine (AChE IC50 = 201.05 nM; BChE IC50 = 202.14 nM) and acarbose (IC50 = 23 124 nM). Among the tested compounds, 6f showed inhibitory activity with IC50 = 119.45 nM (for AChE) and IC50 = 121.58 nM (for BChE), 6v showed inhibitory activity with IC50 = 121.87 nM (for AChE) and IC50 = 118.25 nM (for BChE) and 9g inhibitory activity against α-glucosidase with IC50 = 21 442 nM. The docking and kinetic studies supported the experimental results obtained through in vitro experiments and predicted drug-like properties. [ABSTRACT FROM AUTHOR]

A method for the synthesis of twelve enantiopure derivatives of BEDT-TTF which have two stereogenic centres is reported comprising six diastereomeric pairs. The donors are derivatives of enantiopure (BEDT-TTF)-acetamide bearing a chiral substituent on the nitrogen (NCHMeR: R = 3-Cl-C6H4, 3-OMeC6H4, 4-Me-C6H4, cyclohexyl and 1-naphthyl, and NCH(CH2Ph)CO2Me), and structural assignments are supported by X-ray crystallography. All donors show two successive oxidations typical of BEDT-TTF. Two examples of charge transfer salts with members of this series are reported: a 2 : 1 salt with triiodide in which the anions lie in channels along the donor stacking direction and a 1 : 1 salt with TCNQ-F2 in which the donors and acceptors lie side by side, and staggered with respect to the next layer. Hydrogen bonding between the donors' amide groups is an important feature in the crystal structures. [ABSTRACT FROM AUTHOR]

Clerodendrum trichotomum Thunb. (C. trichotomum) is a shrub or tree of the genus Clerodendrum , family Lamiaceae, which is widely distributed in China, Korea, India, Japan and Philippines. C. trichotomum is a kind of medicinal and edible plant which integrates ecological afforestation, garden greening, herbal medicine and flavor wild vegetable. As a traditional Chinese medicine, C. trichotomum is used to treat various diseases and conditions, which has inspired research on the pharmacological activities of its different parts, including roots, stems, leaves, flowers and fruits. These studies have revealed many biological properties of C. trichotomum , such as antihypertensive, antitumor, antioxidant, antiinflammatory, antibacterial, analgesic, sedative, anti-HIV-1 and whitening. A total of 164 secondary metabolites were isolated from C. trichotomum , and their structural types were mainly terpenoids, flavonoids, steroids, phenylpropanoids and phenylpropanoid glycosides, phenylethanosides, phenolic glycosides, anthraquinones, polyketones, cyclohexylethanoids, alkaloids and acid amides. The presence of a variety of phytochemicals, especially abietane diterpenes, clerodane diterpenes, phenylpropanoid glycosides and flavonoid glycosides, plays an important role in the activity diversity of this plant. The current study is attempt to comprehensively compile information regarding the phytochemicals and pharmacological activities of C. trichotomum , provide the chemotaxonomic proof for the taxonomic classification of the plant, and also highlight the current gaps and propose possible bridges for the development of C. trichotomum as a therapeutic against important diseases. [ABSTRACT FROM AUTHOR]

Singly occupied molecular orbital (SOMO) activation of in situ generated enamines has achieved great success in (asymmetric) a-functionalization of carbonyl compounds. However, examples on the use of this activation mode in the transformations of other functional groups are rare, and the combination of SOMO activation with transition metal catalysis is still less explored. In the area of deoxygenative functionalization of amides, intermediates such as iminium ions and enamines were often generated in situ to result in the formation of a-functionalized amines. In contrast, the direct deoxygenation of amides to ß-functionalized amines is highly appealing yet remains scarcely investigated. Here, a deoxygenative arylation of amides with aryl halides was developed via multicatalysis of iridium/photoredox/nickel/iridium, affording ß-aryl amines in high efficiency. The key to the success of this reaction is the SOMO activation of enamine in synergy with a Ni-catalyzed arylation, which is in conjunction with two compatible Ir-catalyzed reduction processes. [ABSTRACT FROM AUTHOR]

This study explores the development and evaluation of a novel series of aromatic co-polyamides featuring diverse pendant groups, including phenyl and pyridinyl derivatives, designed for water desalination membrane applications. These co-polyamides, synthesized with a combination of hexafluoroisopropyl, oxyether, phenyl, and amide groups, exhibited excellent solubility in polar aprotic solvents, thermal stability exceeding 350 °C, and the ability to form robust, flexible films. Membranes prepared via phase inversion demonstrated variable water permeability and NaCl rejection rates, significantly influenced by the pendant group chemistry. Notably, pyridinyl-substituted membranes achieved water fluxes up to 17.7 L m−2 h−1 and a NaCl rejection of 37.3%, while phenyl-substituted variants provided insights into the interplay of hydrophobicity and porosity. These findings highlight the critical role of pendant group functionality in tailoring membrane performance, offering a foundation for further structural modifications to enhance efficiency in water treatment technologies. [ABSTRACT FROM AUTHOR]

This article aims to review research updates and progress on the nutritional significance of the amides I and II, the alpha-helix and beta-sheet ratios, the microbial protein synthesis, and the steam pressure toasting condition in food and feed with globar and synchrotron molecular microspectroscopic techniques plus chemometrics (both univariate and multivariate techniques). The review focused on (I) impact of the amides I and II, and the alpha-helix and beta-sheet-structure ratios in food and feeds; (II) Current research progress and update in synchrotron technique and application in feed and food molecular structure studies that are associated with nutrition delivery; (III) Impact of thermal processing- steam pressure toasting condition on feed and food; (IV). Impact of the microbial protein synthesis and methodology on feed and food; and (V). Impact on performance and production of ruminants with Faba beans. [ABSTRACT FROM AUTHOR]

Graphene (nano) platelets (GPs) are cost‐effective and possess high structural integrity, but their limited surface functional groups hinder their compatibility with polymers. In this study, an eco‐friendly, water‐based mechanochemical approach was developed to modify GPs with polyacrylamide (PAM), creating PAM graphene platelets (PAM‐GPs) with a grafting ratio of approximately 15%. The platelet was measured to be a few nanometers in thickness, and the grafted PAM provides abundant functional groups, including amide groups, which enhance compatibility with polymers. A typical polymer, bisphenol‐A epoxy, was compounded with PAM‐GPs, resulting in a high degree of exfoliation and dispersion of PAM‐GPs within the matrix. The resulting epoxy/PAM‐GP composites exhibited significantly improved mechanical properties, including an 18% increase in Young's modulus and a substantial enhancement in fracture toughness, with a 71% increase at a low filler fraction of 0.5 wt%. These improvements are attributed to the effective interfacial interaction between the PAM‐GPs and the epoxy matrix, facilitated by the grafted functional groups. This study highlights the potential of PAM‐GPs as toughening fillers for epoxy composites, emphasizing their applicability in enhancing the durability and performance of structural components in industrial applications. Highlights: Polyacrylamide (PAM)‐modified graphene platelets by a water‐based approach.A strong interface promoted exfoliation and dispersion of platelets.PAM‐modified platelets improved epoxy modulus and toughness.Fractographic analysis unveils toughening mechanisms. [ABSTRACT FROM AUTHOR]

Phenolic polymers with catechol groups easily undergo oxidative crosslinking. Through the incorporation of pendant amide groups, the thermal stability of linear phenolic polymers with catechol moieties was significantly improved with maintained antioxidation performance and solubility in THF after storing at 80 8C for 96 hours. [ABSTRACT FROM AUTHOR]

Herein, we report the synthesis of a series of new compounds by combining 2-aminobenzothiazole with various profens. The compounds were characterized using techniques such as 1H- and 13C-NMR, FT-IR spectrometry, and high-resolution mass spectrometry (HRMS), with detailed HRMS analysis conducted for each molecule. Their biological activities were tested in vitro, revealing significant anti-inflammatory and antioxidant effects, comparable to those of standard reference compounds. Lipophilicity was experimentally determined through partition coefficient (RM) measurements. To understand their binding affinity, molecular docking studies were perfsormed to analyze interactions with human serum albumin (HSA). The stability of these predicted complexes was further evaluated through molecular dynamics simulations. The results highlight the compounds' promising biological activity and strong affinity for HSA. The new hybrid molecule between 2-ABT and ketoprofen 3b demonstrates significant promise based on the experimental data and is further supported by in silico calculations. Compound 3b exhibits the best hydrogen peroxide scavenging activity among the tested compounds, with an IC50 of 60.24 μg/mL. Furthermore, 3b also displays superior anti-inflammatory activity, with an IC50 of 54.64 μg/mL, making it more effective than the standard ibuprofen (76.05 μg/mL). [ABSTRACT FROM AUTHOR]

Conversion of quinoline C−H bonds into C−C bonds is essential for obtaining the enormous array of derivatives required for pharmaceutical and agrochemical development. Despite over a century of synthetic efforts, direct alkylation and alkenylation at C3−H positions in a wide array of quinoline precursors remain predominantly challenging and elusive. This report outlines the first successful quinoline C3−H alkylation and alkenylation reactions, exhibiting exceptional regio‐ and stereoselectivity, all achieved under redox‐neutral and transition‐metal‐free conditions. The method involves a three‐step, one‐pot or two‐pot sequence, including 1,4‐dearomative addition, functionalization at C3, and elimination or transalkylation to produce 3‐alkylated/alkenylated quinolines. The presence of a carbonyl group in these products allows for further synthetic manipulations, enabling the production of cyanides, amides, amines, and simple alkyl derivatives. [ABSTRACT FROM AUTHOR]

The article discusses the evolutionary innovations in land plants, focusing on the role of flavonoids in responding to environmental stressors. Flavonoids are highlighted for their multifunctionality, including antioxidant properties and regulation of plant growth and development. The text explores the ancient origins of flavonoids and their diverse roles in plant-environment interactions, emphasizing their ability to modulate oxidative stress signaling pathways. The study also delves into the relationship between flavonoids and abiotic stressors, such as UV radiation, and their involvement in signaling pathways related to auxin and ABA. The article concludes by underscoring the importance of antioxidant flavonoids in plant adaptation to changing environmental conditions. [Extracted from the article]

With the interest and knowing the importance of ferrocenyl conjugates, a direct amidation of ferrocenyl aldehyde has been developed under feasible conditions. Varieties of amines has been oxidatively coupled with ferrocene aldehyde in the presence of highly economical and robustly stable iron chalcogenide ironcarbonyl clusters [Fe3E2(CO)9, E= S, Se, and Te] and TBHP. The reaction worked in greener solvent water at a moderate temperature of 70 °C and the ferrocenyl‐amides in just 30 minutes. All the varieties of amines were found to be well tolerated for the present method, and due to the high medicinal importance of ferrocenyl‐amides, sole focus of this report was concentrates on the synthesis of various new ferrocenyl‐amides in good to excellent amounts. [ABSTRACT FROM AUTHOR]

Context.--New-generation antiseizure medications (ASMs) are increasingly prescribed, and therapeutic drug monitoring (TDM) has been proposed to improve clinical outcome. However, clinical TDM data on new-generation ASMs are scarce. Objective.--To develop and validate a liquid chromatography- tandem mass spectrometry (LC-MS/MS) method for therapeutic drug monitoring (TDM) of 6 new-generation ASMs in serum and analyze the clinical TDM data from a large cohort of Korean patients with epilepsy. Design.--Stable isotope-labeled internal standards were added to protein precipitations of serum. One microliter of sample was separated on an Agilent Poroshell EC-C18 column, and lacosamide, perampanel, gabapentin, pregabalin, vigabatrin, and rufinamide were simultaneously quantified by Agilent 6460 triple-quad mass spectrometer in multiplereaction monitoring mode. Linearity, sensitivity, precision, accuracy, specificity, carryover, extraction recovery, and matrix effect were evaluated. TDM data of 458 samples from 363 Korean epilepsy patients were analyzed. Results.--The method was linear with limit of detection less than 0.05 lg/mL in all analytes. Intraassay and interassay imprecisions were less than 5% coefficient of variation. Accuracy was within 615% bias. Extraction recovery ranged from 85.9% to 98.8%. A total of 88% (403 of 458) were on polypharmacy, with 29% (118 of 403) using concomitant enzyme inducers. Only 38% (175 of 458) of the concentrations were therapeutic, with 53%(244 of 458) being subtherapeutic. Drug concentration and concentration-to-dose ratio were highly variable among individuals for all 6 ASMs. Conclusions.--A simple and rapid LC-MS/MS method for TDM of 6 ASMs was developed and successfully applied to clinical practice. These large-scale TDM data could help establish an effective monitoring strategy for these drugs. [ABSTRACT FROM AUTHOR]

Comprehensive Summary Here, we show a cost‐effective and environmentally friendly method for synthesizing iminofuranones using visible light and the photocatalyst 2‐bromoanthraquinone. Our approach uses only oxygen as the oxidant, avoiding the need for additional transition metals and strong oxidizing agents. By employing a mixed solvent system of DMF and CHCl3 under ambient conditions, we have achieved highly diastereoselective conversions of various 2‐vinyl benzamides and alkenyl amides into functionalized iminoisobenzofuranones and iminofuranones. This versatile process is broadly applicable and enables late‐stage structural modifications of complex substrates with bioactive moieties. [ABSTRACT FROM AUTHOR]

The synthesis of 2‐(pentafluoro‐λ6‐sulfanyl)acetamides is described via an amidation reaction between 2‐(pentafluoro‐λ6‐sulfanyl)acetic acid, the SF5‐containing building block, and various amines. A total of 27 examples of SF5‐containing amides were synthesized, with isolated yields going from 43 % to quantitative. We showed that a 2‐(pentafluoro‐λ6‐sulfanyl)acetamide could be converted to a N‐(2‐SF5‐ethyl)amine and a SF5‐containing oxadiazoles. Finally, the effect of the SF5 substituent on the lipophilicity of the amide of a model compound was evaluated. [ABSTRACT FROM AUTHOR]

The discovery and optimisation of reaction conditions leading to the reduction of amides, a fundamental large-scale industrial reaction, is achieved using a machine learning (ML) platform and a platinum catalyst. The optimisation leads to the discovery of a new platinum-based catalytic system that displays unexpectedly high performance. The approach enables rapid and high conversions at ppm-level catalyst loadings. [ABSTRACT FROM AUTHOR]

Despite the preliminary success of transition metal‐catalyzed [3+2] annulation of amides with olefins, the corresponding radical‐type [3+2] annulation remains a laborious challenge. Herein we report the first photoredox‐catalyzed radical‐type [3+2] annulation of aromatic amides with olefins. We established an approach to generate unprecedented iminium radicals by reducing the oxyiminium intermediates, formed in situ from corresponding amides with Tf2O, via photoredox catalysis. The [3+2] annulation was achieved via stepwise radical process, instead of forming linear products via other pathways as previously reported. This annulation protocol exhibits excellent functional group tolerance, and a diversity of substrates are united under the photoredox conditions, affording iminium products that can be in situ diversified into 1‐indanones, enamines and amines. Mechanistic investigations indicate reduction of the oxyiminium intermediate to the iminium radicals by excited‐state of the photocatalyst initiates the catalytic cycle. [ABSTRACT FROM AUTHOR]

Expanding the library of structurally characterized lithium amidomanganates(II), here we report a general synthetic approach to access a new series of homoleptic complexes. In situ salt‐metathesis of commercially available reagents afforded tetrabutyl lithium manganate [(TMEDA)2Li2Mn(nBu)4] (1) (TMEDA=N,N,N',N'‐tetramethylethylendiamine) which could be used as a precursor for direct deprotonation of a selection of amines affording a family of homoleptic lithium amidomanganates. Complexes [{Li(THF)4}+{Mn(NPh2)3(THF)}‐] (2), [(THF)LiMn(NCy2)3] (3) (Cy=cyclohexyl), [(HNCy2)LiMn(NCy2)3] (4), [(THF)4Li2Mn(NHMes)4] (5) (Mes=2,4,6‐trimethylphenyl), and [(TMEDA)2Li2Mn(NHMes)4] (6) have been isolated and structurally characterized as main products. While it is evident that 1 possesses adequate basicity to effect deprotonation of both primary and secondary amines, the exact stoichiometry, constitution, and structural motif of newly generated lithium amidomanganates are governed by the steric and electronic variations of the amide ligands. [ABSTRACT FROM AUTHOR]

KAR (Karrikin), a novel plant growth regulator, can be recognized specifically by plants and can activate resistance responses. MdKAI2 is the natural receptor of KARs in apple. Here, we report the identification of osmotic stress resistance in MdKAI2 via the method of genetic transformation. The phenotypic traits, resistance indicators, and transcriptional and metabolic regulation of MdKAI2 were identified. KAR1, a highly active form of KAR, markedly promoted the root growth of Gala cultivar tissue culture‒generated plants, possibly through increases in ABA and TZR contents and decreases in the GA3 content. MdKAI2 was markedly upregulated by PEG stress and significantly promoted the growth of apple calli under nonstress conditions, whereas it was significantly inhibited under 20% PEG stress, as was cell death. MdKAI2 significantly increased the content of total flavonoids, the activity of reactive oxygen species (ROS)‒scavenging enzymes (SOD, POD and CAT), and the content of osmoregulatory substances (soluble protein, soluble sugars and proline). It also inhibited the MDA content and conductivity under osmotic stress. Differentially expressed genes (DEGs), including multiple transcription factors (TFs), such as MYB , bHLH and AP2‒EREBP , are significantly regulated by MdKAI2, and genes involved in the mitogen‒activated protein kinase (MAPK) signaling pathway play crucial roles in the regulation of plant resistance. In addition, pathways such as brassinosteroid (BR) biosynthesis and ABC transporters were downregulated, and the MAPK signaling pathway; plant‒pathogen interaction; cutin, suberin and wax biosynthesis; alpha‒linolenic acid metabolism; and phenylpropanoid biosynthesis were upregulated by MdKAI2. MdKAI2 significantly regulates the levels of lipids, amino acids, terpenoids, benzene, organic acids, carbohydrates, and alkaloids and is involved in the metabolic processes of amino acids, carbohydrates, nucleotides, lipids and secondary metabolites. Furthermore, MdKAI2 positively regulates fatty acids, esters, and terpenoids and negatively regulates metabolites of amino acids, amides and alcohols, and the MAPK signaling pathway may mediate this process. The study has provided a new direction for the industrial application of KAR1 in apples and resistance breeding based on the gene of MdKAI2. [ABSTRACT FROM AUTHOR]

Introducing two electron-donating groups and two electron-withdrawing groups together in symmetrical positions on the benzene ring is a fundamental way to synthesize and prepare single-benzene-based fluorophores (SBBFs). Their photophysical properties are adjusted through the electronic and structural properties of the functional groups. Reported herein is the functionalization of diaminobenzene derivatives with various amine protecting groups, including amides, urea, carbamates, and sulfonamides. Both absorption and emission properties of the obtained SBBF molecules were carefully investigated. Sequential and unsymmetric diamine protections were also explored with diaminobenzene derivatives for fine-tuning of the molecular properties. [ABSTRACT FROM AUTHOR]

Acute kidney injury (AKI) is a critical condition with a wide range of triggers that cause heavy burden on public health. Despite its high incidence and mortality, the treatment of AKI still highly relies on hemodialysis, which is costly and usually accompanied by severe complications. Therefore, development of new therapeutic targets and methods for AKI is urgently needed. Herein, a ferroptosis‐targeting strategy for AKI treatment by rationally designed ferroptosis‐inhibitive polypeptide‐based polymersomes (polypeptosomes, FIPs) is proposed. Such FIPs are self‐assembled from poly(glutamic acid)‐block‐poly(methionine‐stat‐tyrosine) [PGA9‐b‐P(Met8‐stat‐PTyr13)]. The ferroptosis‐inhibition function of the FIPs arises from the rationally‐selected amino acid composition: P(Met‐stat‐Tyr) endows the FIPs with a high scavenging efficiency of over 90% toward different reactive oxygen species (ROS); while the glutamate and tyrosine residues, as well as the amide groups, can bind iron ions, thus blocking iron overload and lipid peroxide in cells. In vivo experiments confirm that the FIPs can effectively alleviate oxidative stress, inhibit ferroptosis, and restore kidney functions. Transcriptome sequencing further reveals the therapeutic mechanisms of FIPs. Overall, such polypeptosomes capable of blocking multiple pathways of ferroptosis open a new avenue for AKI treatment and provide fresh insights into the development of generalized therapies for inflammation. [ABSTRACT FROM AUTHOR]

N,O-hybrid donor ligands are promising compounds for the isolation and separation of actinides and lanthanides from process solutions of spent nuclear fuel reprocessing. Newly synthesized N,O-hybrid donor ligands – derivatives of 2,6-pyridinedicarboxylic acid were studied as extractants and membrane components for potentiometric sensors. The extraction ability of solutions of these compounds in meta-nitrobenzotrifluoride towards d- and f-elements from nitric and perchloric acid solutions was investigated. It was shown that the replacement of amide groups with ester groups reduces the extraction ability of the ligands. Switching from nitric acid to perchloric acid gives a dramatic increase in extraction capacity due to the perchlorate effect. Also, a significant increase in extraction capacity is observed when chlorinated cobalt dicarbolide is added to the organic phase: the highest distribution coefficient is observed at a 1 : 1 ratio of extractant and additive concentrations. Potentiometric membrane sensors based on the new ligands showed significant sensitivity to Cd2+. Correlations between extraction and sensing behavior of new ligands were studied. [ABSTRACT FROM AUTHOR]

We present a novel and cost-effective method for synthesizing biologically important α-keto esters in a single-step reaction. This approach involves a sequential cascade process within a single reaction vessel facilitated by t -BuOK, which promoted the cleavage of the sp2 C(O)–N bond of an isatin and the formation of a new N–C(sp2)(O) bond with benzoyl chloride. To the best of our knowledge, this is the first instance of the construction of an α-keto ester scaffold adjacent to an amide group through a one-pot process. In comparison to existing methods, our protocol offers several advantages: readily available starting materials, mild reaction conditions, a concise synthetic pathway, high sustainability, and excellent tolerance towards various functional groups. Given these strengths, we anticipate widespread use of this method in the synthesis of related α-keto ester scaffolds. [ABSTRACT FROM AUTHOR]

N -Formylation of anilines using a renewable aleuritic acid as an eco-friendly and sustainable formylating source has been developed. para -Substituted anilines generally provided good yields, while moderate yields were observed with meta - and ortho -substituted derivatives. In situ generated formic acid through oxidative cleavage of aleuritic acid serve as a formyl source, which has been confirmed through control experiments. [ABSTRACT FROM AUTHOR]

A multi‐gram scale synthesis of ferrocenetriflone was optimised from ferrocenesulfonyl fluoride and Me3SiCF3 (Ruppert reagent). Enantioselective deprotolithiations were then optimised using alkyllithiums in the presence of catalytic (+)‐sparteine to afford 2‐substituted ferrocene triflones in 79–84% ee. The use of chiral lithium amides in the presence of in situ traps was also optimised and was found to outperform alkyllithium⋅chiral diamine chelates for the first time in the ferrocene series, with 89–93% ee. Crystallisation of derivatives afforded enantiopure compounds that were engaged in deprotolithiation‐electrophilic trapping sequences, a halogen 'dance' reaction and transition metal‐promoted coupling to afford a wide range of variously polysubstituted ferrocene triflones. [ABSTRACT FROM AUTHOR]

When γ,δ‐epoxy‐α,β‐unsaturated esters were treated with 3 equiv. of aliphatic Grignard reagents in the presence of 10 and 20 mol% FeCl2 and N,N,N',N'‐tetramethylethylenediamine, regio‐ and stereoselective substitution of the epoxide moiety with the aliphatic Grignard reagent occurred, producing exclusively δ‐hydroxy‐γ‐alkyl‐α,β‐unsaturated esters. Similarly, γ,δ‐epoxy‐α,β,ϵ,ζ‐unsaturated esters and amides underwent transformation to the corresponding δ‐hydroxy‐γ‐alkyl‐α,β,ϵ,ζ‐unsaturated esters and amides as single isomers, respectively. [ABSTRACT FROM AUTHOR]

Chiral macrocycles have emerged as attractive media for chromatographic enantioseparation due to their excellent host‐guest recognition properties. In this study, a new chiral stationary phase (CSP) based on 1,1'‐binaphthyl chiral polyimine macrocycle (CPM) was reported. The CPM was synthesized by one‐step aldehyde‐amine condensation of (S)‐2,2'‐dihydroxy‐[1,1'‐binaphthalene]‐3,3'‐dicarboxaldehyde with 1,2‐phenylenediamine and bonded on thiolated silica via the thiol‐ene click reaction to afford the CSP. The enantioseparation performance of the CSP was evaluated by separating different types of racemates including alcohols, esters, ketones, amides, organic acids, and ethers in both normal‐phase (NP) and reversed‐phase (RP) elution modes. As a result, enantioseparations of 10 and 15 racemates were achieved in the two elution modes, respectively. Meanwhile, the effects of chromatographic conditions on separation, such as mobile phase composition and injection mass, were studied in detail. Moreover, a comparison of the proposed CSP for the separation of the tested racemates with commercial Chiralcel OD‐H and Chiralpak AD‐H columns was also conducted, and results revealed that the proposed CSP can achieve some enantioseparations that cannot be achieved by the two commercial columns. This study indicates that the chiral macrocycle is a promising chiral selector for high‐performance liquid chromatography. [ABSTRACT FROM AUTHOR]

Comprehensive Summary: The difunctionalization of bicyclo[1.1.0]butanes is an under‐explored transformation that accesses to moieties that are otherwise difficult to prepare. Herein, a new oxidative radical alkylarylation of N‐aryl bicyclobutyl amides with C(sp3)−H feedstocks is achieved in an atom‐economic and photocatalyst‐ and light‐free manner. This protocol follows a sequential C(sp3)–H/C(sp2)–H functionalization, providing an efficient route for diversity‐oriented synthesis of functionalized 3‐spirocyclobutyl oxindoles. In particular, a wide range of C(sp3)−H feedstocks, including ether, alcohol, amine, thioether, polychlorinated methane, silane, acetone, acetonitrile, toluene, and alkane are all suitable for the C(sp3)−H functionalization, demonstrating the broad applicability of this transformation. [ABSTRACT FROM AUTHOR]

Comprehensive Summary: Catalytic methylative coupling of internal alkynes and aldehydes/aldimines through regioselective oxidative cyclization promoted by a phosphine–Co complex is presented. Such process constitutes an unprecedented and unique approach for Co‐catalyzed generation of metallacycles that reversed inherent regiochemical biases to furnish a wide range of allylic alcohols and allylic amides bearing a tetrasubstituted alkene in up to 98% yield with high regioselectivity, representing a novel and general strategy for reversal of substrate‐controlled regioselectivity in metal‐catalyzed oxidative cyclization. [ABSTRACT FROM AUTHOR]

Comprehensive Summary: Boronate esters are highly valued in synthetic and pharmaceutical industries for their versatility in creating C—C and C—X bonds. They also find applications as catalysts in chemical transformations as well as stimuli‐responsive materials in materials science. Some alkyl boronates themselves also show promising applications in medicinal chemistry. In the past few decades, chemists have been devoted to developing new methods or new starting materials for synthesizing boronate esters. Carboxylic acids and their derivatives are privileged chemical entities due to their readily availability or natural abundance, structural diversity, and chemical stability. Hence, the transformation of carboxylic acid and their derivatives to alkyl/aryl boronate esters has seen its fast development in the past decade. This review summarized the state‐to‐art development of decarboxylative and decarbonylative borylation of carboxylic acids and their derivatives to aryl and alkyl boronate esters. Key Scientists: The decarboxylative and decarbonylative borylation of carboxylic acids and their derivatives started only in the past decade. In 2016, the decarbonylative borylation of carboxylic esters and amides was reported by Zhuangzhi Shi and Magnus Reuping's groups. Then, in 2017, studies on the decarboxylative borylation of redox‐active esters such as NHPI esters started to receive increasing attention by Aggarwal, Baran, Fu, Glorius, and Li's groups. From 2018 to 2023, large numbers of studies on the decarboxylative and decarbonylative borylation of carboxylic acids and their derivatives using transition‐metal‐catalyst, organo‐catalyst, or under photochemical or electrochemical conditions emerged. Due to space limitations, only pictures of scientists who have contributed more than two works in this area are shown herein. [ABSTRACT FROM AUTHOR]

An efficient Pd(II)‐catalyzed remote selective cross‐dehydrogenative coupling of broadly useful synthetic building blocks biphenyl Weinreb amides with carboxylic acids is developed. This acetoxylation protocol is performed under room temperature using N‐fluorobenzene‐sulfonimide (NFSI) as the oxidant, exhibiting a wide range of functional group tolerance and affording δ‐position‐ selective products up to 85 % yield. Notably, a diverse set of carboxylic acid‐containing drugs is also found to be compatible under the current reaction conditions. Preliminary mechanistic studies indicate that this reaction presumably proceeds through a seven‐membered palladacycle intermediate. [ABSTRACT FROM AUTHOR]

A metal‐free α‐(hetero)arylation of aryloxy‐activated amides for access to diaryl‐acetamides was developed. This base‐mediated arylation reaction features mild reaction conditions and broad functional groups tolerance. The scope of (hetero)arylating reagents includes indoles, pyrroles, furan, N, N‐dimethylanilines, and electron‐rich benzenes. The applicability of this protocol was demonstrated by the gram‐scale experiment and the derivatization of the target products. [ABSTRACT FROM AUTHOR]

Comprehensive Summary: Boronate esters are highly valued in synthetic and pharmaceutical industries for their versatility in creating C—C and C—X bonds. They also find applications as catalysts in chemical transformations as well as stimuli‐responsive materials in materials science. Some alkyl boronates themselves also show promising applications in medicinal chemistry. In the past few decades, chemists have been devoted to developing new methods or new starting materials for synthesizing boronate esters. Carboxylic acids and their derivatives are privileged chemical entities due to their readily availability or natural abundance, structural diversity, and chemical stability. Hence, the transformation of carboxylic acid and their derivatives to alkyl/aryl boronate esters has seen its fast development in the past decade. This review summarized the state‐to‐art development of decarboxylative and decarbonylative borylation of carboxylic acids and their derivatives to aryl and alkyl boronate esters. Key Scientists: The decarboxylative and decarbonylative borylation of carboxylic acids and their derivatives started only in the past decade. In 2016, the decarbonylative borylation of carboxylic esters and amides was reported by Zhuangzhi Shi and Magnus Reuping's groups. Then, in 2017, studies on the decarboxylative borylation of redox‐active esters such as NHPI esters started to receive increasing attention by Aggarwal, Baran, Fu, Glorius, and Li's groups. From 2018 to 2023, large numbers of studies on the decarboxylative and decarbonylative borylation of carboxylic acids and their derivatives using transition‐metal‐catalyst, organo‐catalyst, or under photochemical or electrochemical conditions emerged. Due to space limitations, only pictures of scientists who have contributed more than two works in this area are shown herein. [ABSTRACT FROM AUTHOR]

(1) Background: Carbapenem-resistant Acinetobacter baumannii (CBRAB) and Pseudomonas aeruginosa (CBRPA) are critical and high-priority pathogens that require new therapeutic developments. Medicinal plants are valuable pharmaceutical resources. This study explored the anti-infective properties of Mayan plants, Bignonia potosina, and Thouinia paucidentata. (2) Methods: Plant parts were extracted using n-hexane, and their ability to inhibit bacterial growth and counteract resistance mechanisms and virulence factors in CBRAB and CBRPA was assessed. GC-MS analysis of the composition of the non-polar extracts and chemometric techniques correlated the phytoconstituents with anti-infective properties. (3) Results: Bignonia potosina liana and flower extracts exhibited potent antibacterial activity against A. baumannii strains (MIC 15.7 to 250 µg/mL) and moderate activity against P. aeruginosa strains (MIC 250 to 1000 µg/mL). Thouinia paucidentata leaf extract at 1000 µg/mL reduced imipenem MIC by 2048-fold for CBRAB, and B. potosina flower extract significantly inhibited A. baumannii catalase activity (at 62.5 µg/mL) and reduced P. aeruginosa pyocyanin production (at 1000 µg/mL). Chemometric analysis identified fatty acids, fatty acid amides, terpenes, and higher alkanes as contributors to their anti-infective properties. (4) Conclusions: This study highlights the potential of medicinal plants in the development of novel anti-infective therapies against CBRAB and CBRPA with various targets. [ABSTRACT FROM AUTHOR]

A mild and efficient strategy to synthesize pharmaceutically important 3-amino oxindoles from readily available N-aryl amides has been developed. This unique reaction proceeds via the intramolecular cyclization of 2-azaallyl anions with N-aryl amides to afford 3-amino substituted oxindoles. This novel method avoids the direct usage of transition metal catalysts and additional oxidants. Furthermore, the anti-pulmonary fibrosis activity evaluation showed that 3-amino oxindole 2f significantly inhibited collagen deposition, which can ameliorate pulmonary fibrosis by reducing excessive extracellular matrix (ECM) deposition. [ABSTRACT FROM AUTHOR]

Unsymmetrically N,N'‐substituted metal amides of silicon, germanium and aluminium were synthesized starting from N‐ethyl‐2‐(n‐propylaminomethyl)phenylamine (1, Et,nPr‐ampaH2). Reaction of the dilithium compound of 1 with SiCl4 gave spirocyclic Si(Et,nPr‐ampa)2 (2) and Cl2Si(Et,nPr‐ampa) (3). Reduction of 3 with potassium resulted in the formation of the corresponding cyclotetrasilane [Si(Et,nPr‐ampa)]4 (4), whereas the reaction of 3 with lithium triethylborohydride gave the dihydro silane H2Si(Et,nPr‐ampa) (5). The corresponding germanium(IV) compounds Ge(Et,nPr‐ampa)2 (6) and Cl2Ge(Et,nPr‐ampa) (7) were synthesized starting from GeCl4, amine 1 and NEt3 using appropriate stoichiometric ratios. Reaction of Ge[N(SiMe3)2]2 with amine 1 provided the germylene [Ge(Et,nPr‐ampa)]2 (8). The aluminium dichloro compound Cl2Al(Et,nPr‐ampaH) (9) was obtained either by reaction of the dichlorogermine 7 with lithium aluminium hydride or by reaction of the dilithium salt of 1 with AlCl3. Reaction of trimethylaluminium with amine 1 provided the amido‐amine (CH3)2Al(Et,nPr‐ampaH) (10) which was converted into the diamide CH3Al(Et,nPr‐ampa) (11) by methane elimination. [ABSTRACT FROM AUTHOR]

The direct asymmetric vinylogous allylic alkylation is an efficient method to construct chiral 1,5‐diene compounds. In this work, acyclic unsaturated amides are used as a nucleophile for enantioselective vinylogous allylic alkylation. With 10 mol % of chiral tertiary amine C11, the enantioselective vinylogous allylic alkylation between β,γ‐unsaturated pyrazoleamides and Morita‐Baylis‐Hillman carbonates is achieved, affording optically active multifunctional chiral 1,5‐dienes in moderate‐to‐excellent yields (74–99 %) with good‐to‐excellent enantioselectivities (67–94 % ee). [ABSTRACT FROM AUTHOR]

In this work, we developed a visible‐light‐driven method for the selective synthesis of amides and N‐acylureas from carboxylic acids and thioureas. This protocol was featured as avoidance of additional oxidants and transition metal catalysts, simple manipulations, low cost, broad substrate scope, and good functional group tolerance. As only oxygen serves as the oxidation reagent, this method provides a promising synthesis candidate for the formation of N‐aryl amides and N‐acylureas, including late‐stage functionalization of complex pharmaceutical molecules and biologically active molecules. [ABSTRACT FROM AUTHOR]