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aims: Greener Synthesis and biological evaluation of some novel dispiroheterocycles background: The increasing utilization of spiro compounds in drug discovery, led us to design and synthesize regioselectively some novel dispiroheterocycles, by a standard 1,3-dipolar cycloaddition reaction between 6-hydroxyaurone and in situ generated azomethine ylides, using ultra-sonication as green energy source. These results are first of its kind in the literature reported so far for the similar conditions. After confirmation of the proposed structures spectroscopically, using 1H NMR, 13C NMR and FT-IR spectral data, all the compounds are screened for their potential biological activities. objective: To develop greener protocol for the synthesis of dispiroheterocycles and their biological evaluation method: Three component protocol, that contains (Z)-2-benzylidene-6-hydroxybenzofuran-3(2H)-one, sarcosine and unsubstituted isatin. In which azomethine ylides react with olefinic dipolarophiles through 1,3-dipolar cycloaddition which is highly regio- and stero-selective way in situ. Structures of the proposed products have been confirmed using 1H NMR, 13C NMR and FT-IR spectral data. result: In order to screen the potential biological activities of the synthesized compounds their effect was observed on trypsin, amylase and lipase activities. Differential effect has been observed. Trypsin was substantially activated whereas an inhibitory effect was observed for amylase and lipase supported by in-silico studies. conclusion: Synthesis of six novel 6-hydroxy-1'-methyl-4'-phenyl-3H-dispiro[benzofuran-2,3'-pyrrolidine-2',3''-indoline]-2'',3-dione derivatives have been made using a multicomponent greener protocol. These synthesized compounds have exhibited differential effect toward trypsin, amylase and lipase well supported by in-silico studies. Thus the present study highlight their potential use as anti-inflammatory, anti-obesity agents. other: Characterization and enzymatic study of the synthesized novel dispiroheterocycles

Over the past few decades, the dynamic progress in the synthesis and screening of heterocyclic compounds against various targets has made a significant contribution in the field of medicinal chemistry. Among the wide array of heterocyclic compounds, triazole moiety has attracted the attention of researchers owing to its vast therapeutic potential and easy preparation via copper and ruthenium-catalyzed azide-alkyne cycloaddition reactions. Triazole skeletons are found as major structural components in a different class of drugs possessing diverse pharmacological profiles including anti-cancer, anti-bacterial, anti-fungal, anti-viral, anti-oxidant, anti-inflammatory, anti-diabetic, anti-tubercular, and anti-depressant among various others. Furthermore, in the past few years, a significantly large number of triazole hybrids were synthesized with various heterocyclic moieties in order to gain the added advantage of the improved pharmacological profile, overcoming the multiple drug resistance and reduced toxicity from molecular hybridization. Among these synthesized triazole hybrids, many compounds are available commercially and used for treating different infections/disorders like tazobactam and cefatrizine as potent anti-bacterial agents while isavuconazole and ravuconazole as anti-fungal activities to name a few. In this review, we will summarize the biological activities of various 1,2,3-triazole hybrids with copious oxygen-containing heterocycles as lead compounds in medicinal chemistry. This review will be very helpful for researchers working in the field of molecular modeling, drug design and development, and medicinal chemistry.

The identification of x-ray crystal structure of cathepsin B (CTSB) in the early 90's enabled researchers to embark on a journey to understand and demystify its multiple catalytic mechanisms (endopeptidase/carboxypeptidase/peptidyl-dipeptidase) in diverse physiological processes and their switching into one another under different conditions. The engagement of CTSB in different pathological conditions due to its over-expression further highlighted the enhanced research interest around the domain. The occurrence of over-expressed CTSB in various diseases like Alzheimer's, cancer, arthritis, cardiovascular, etc., and the use of CTSB inhibitors for the treatment of these diseases have established its involvement in different pathological conditions. Such an understanding tempted researchers to design, synthesize, and screen diverse classes of compounds against CTSB. This in turn, helped in understanding their interactions with the active sites of the enzyme. Heterocyclic compounds comprise a very rich and broad class of medicinally important compounds that also hold great potential for CTSB inhibition. This review covers the CTSB inhibition potential of various natural and synthetic heterocyclic scaffolds. Researchers working in the fields of molecular modeling, drug design and development, and enzyme inhibitors can benefit significantly from this review.

The dynamic growth in green organic synthetic methodologies for diverse heterocyclic scaffolds has substantially contributed to the field of medicinal chemistry over the last few decades. The use of hybrid metal nanocatalysts (NCs) is one such benign strategy for ensuring the advancement of modern synthetic chemistry by adhering to the principles of green chemistry, which call for a sustainable catalytic system that converts reacting species into profitable chemicals at a faster rate and tends to reduce waste generation. The metal nanoparticles (NPs) enhance the exposed surface area of the catalytic active sites, thereby making it easier for reactants and metal NCs to have an effective interaction. Several review articles have been published on the preparation of metal NCs and their uses for various catalytic heterocyclic transformations. This review will summarize different metal NCs for the efficient green synthesis of various O-heterocycles. Furthermore, the review will provide a concise overview of the role of metal NCs in the synthesis of O-heterocycles and will be extremely useful to researchers working on developing novel green and simple synthetic pathways to various O-heterocyclic-derived molecules.

A two-step synthesis was designed to develop a novel series of 6-propynyloxyaurones, 2(a-r). The synthesized aurone derivatives were characterized by their IR, NMR, and mass spectrometry data. The present study proposes these aurones as anti-inflammatory and anti-Alzheimer candidates on the basis of their cathepsin B inhibitory activities. Anti-cathepsin B activity of some of the synthesized aurones was found, either equivalent to or higher than the reference drugs, aspirin and curcumin at submicromolar concentrations. Among the studied compounds, 2e, 2i, 2n, 2q, and 2r exhibited much higher activity in comparison to the standard drugs. The molecular docking study also highlighted compound 2r for its greater anti-cathepsin B activity among all the designed aurones.

A series of pyrazole based aurone analogs 3(a-n) have been synthesized and evaluated for their cytotoxic activity against MCF-7 cell line. All the products have been obtained by solid phase reaction and organic solvent free simple work-up procedure. Structures of the synthesized aurones were confirmed by their IR, 1H NMR, 13C NMR, elemental analysis and mass spectrometry data. The cytotoxic activity of these compounds was assessed by MTT assay and the nine products were found to be potential inhibitors against human breast adenocarcinoma cell line i.e. MCF-7. Aurone analogs 3a, 3b, 3c, 3e, 3i and 3n are the most active against the MCF-7 cell line with IC50 of 13.8, 15.8, 4.3, 2.7, 12.9 and 15.5 μg/mL respectively, as compared to paclitaxel, with an IC50 value of 18.5 μg/mL. Cytotoxicity against MCF-7 cancer cells, makes these molecules attractive candidates for the potential anticancer drug.