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A biosensitive analysis method development and validation was performed for accurate and rapid quantification of cefdinir (CDR) in human plasma by a liquid chromatography–tandem mass spectrometry technique coupled with electrospray ionization. Analysis was carried out using a C18 column with a flow rate of 1.0 mL/min and operating temperature of 30.0 ± 1°C. The drug was eluted by optimizing the m/z ratios of 396.20 → 227.20 and 428.17 → 241.10, for cefdinir and IS (internal standard), respectively. The intraday precision (%CV) for Cefdinir ranged from 2.8% and 6.7% as lower limit of quantification of quality control (LLOQ QC) and higher level of quantification of quality control (HQC QC), respectively, whereas these value were found to be as 3.0% and 5.6% for LLOQ and HQC, respectively after interday precision. Moreover, accuracy ranged from 107.70% (HQC QC) to 95.5% (LLOQ QC). The extraction mean recovery was found to be 83.91 ± 6.0% for cefdinir and 76.7 ± 6.23% for IS. The drug was stable throughout the analysis period. It was possible to analyze several plasma samples every day since each sample took <2.5 min to run. The method demonstrated successful quantification of CDR in human plasma, followed by pharmacokinetic profiles that were simple, accurate, sensitive and cost-effective. [ABSTRACT FROM AUTHOR]

The lumpy skin disease (LSD) virus of the Poxviridae family is a serious threat that mostly affects cattle and causes significant economic loss. LSD has the potential to spread widely and its rapidly across borders. Despite the availability of information, there is still no competitive vaccine available for LSD. Therefore, the current study was conducted to develop an epitope-based LSD vaccine that is efficient, secure, and biocompatible and stimulates both innate and adaptive immune responses using immunoinformatics techniques. Initially, putative virion core proteins were manipulated; B-cell and T-cell epitopes have been predicted and connected with the help of adjuvants and linkers. Numerous bioinformatics methods, including antigenicity testing, transmembrane topology screening, allergenicity assessment, conservancy analysis, and toxicity evaluation, were employed to find superior epitopes. Based on promising vaccine candidates and immunogenic potential, the vaccine design was selected. Strong interactions between TLR4 and TLR9 and the anticipated vaccine design were revealed by molecular docking. Finally, based on the high docking score, computer simulations were performed in order to assess the stability, efficacy, and compactness of the constructed vaccine. The simulation outcomes showed that the polypeptide vaccine design was remarkably stable, with high expression, stability, immunogenic qualities, and considerable solubility. Additionally, computer-based research shows that the constructed vaccine provides adequate population coverage, making it a promising candidate for use in the design of vaccines against other viruses within the Poxviridae family and potentially other virus families as well. These outcomes suggest that the epitope-based vaccine developed in this study will be a significant candidate against LSD to control and prevent LSDV-related disorders if further investigated experimentally. [ABSTRACT FROM AUTHOR]

Tectona grandis L.f is a timber plant that is commonly referred to as teak. Its wide use as a medicine in the various indigenous systems makes it a plant of importance. A wide gamut of phytoconstituents like alkaloids, phenolic glycosides, steroids, etc. has been reported. A renewed interest in this plant has resulted in scientific investigations by various researchers towards the isolation and identification of active constituents along with scientific proof of its biological activities. The different parts of the plant have been scientifically evaluated for their antioxidant, antipyretic, analgesic, hypoglycemic, wound healing, cytotoxic, and many more biological activities. Documentation of this scientific knowledge is of importance to have consolidated precise information encompassing the various aspects of this plant, which could provide a base for future studies. This review is a compilation of the salient reports on these investigations concerning phytochemistry, the methods used to identify and quantify the constituents, the evaluation methods of the biological activity, toxicological studies, allergies and the patent/patent applications. This will further help researchers to find an area of the gap for future studies. [ABSTRACT FROM AUTHOR]

Pyridazine derivatives represent one of the most active classes of compounds possessing a wide spectrum of biological activity. They are widely used in pharmaceuticals and agrochemicals. In view of these facts and in continuation of our interest in the chemistry of pyridazines, pyridazinones are six membered cyclic 1,2-diazine having carbonyl group at 3-position of ring system. They are widely used for industrial purposes and also exhibit a broad range of biological activities. This short review compiles examples of the most promising antibacterial activity. An overview on the antifungal activity is also described. [ABSTRACT FROM AUTHOR]

Hydrazones possess an azomethine -NHN=CH group and are considered as derivatives of aldehydes and ketones in which the oxygen atom has been replaced by the NNH2 functional group. These are widely studied molecules owing to their ease of preparation and diverse pharmacological potential. This has led researchers to synthesize different heterocyclic compounds bearing hydrazones. Medicinal chemists across the world have done immense work on hydrazones and developed agents with better activity and low toxicity profiles. Following different synthetic protocols and through proper SAR studies differently substituted hydrazones have been developed and found to be active against different pharmcological targets. They are known to possess different biological activities viz. antimicrobial, antiinflammatory, anticancer, antimalarial etc. These observations can be used as guidance for the development of new hydrazones that possess various biological activities. The review aims to highlight the diverse biological activities of hydrazones. [ABSTRACT FROM AUTHOR]

The COVID-19 pandemic needs no introduction at present. Only a few treatments are available for this disease, including remdesivir and favipiravir. Accordingly, the pharmaceutical industry is striving to develop new treatments for COVID-19. Molnupiravir, an orally active RdRp inhibitor, is in a phase 3 clinical trial against COVID-19. The objective of this review article is to enlighten the researchers working on COVID-19 about the discovery, recent developments, and patents related to molnupiravir. Molnupiravir was originally developed for the treatment of influenza at Emory University, USA. However, this drug has also demonstrated activity against a variety of viruses, including SARS-CoV-2. Now it is being jointly developed by Emory University, Ridgeback Biotherapeutics, and Merck to treat COVID-19. The published clinical data indicate a good safety profile, tolerability, and oral bioavailability of molnupiravir in humans. The patient-compliant oral dosage form of molnupiravir may hit the market in the first or second quarter of 2022. The patent data of molnupiravir revealed its granted compound patent and process-related patent applications. We also anticipate patent filing related to oral dosage forms, inhalers, and a combination of molnupiravir with marketed drugs like remdesivir, favipiravir, and baricitinib. The current pandemic demands a patient compliant, safe, tolerable, and orally effective COVID-19 treatment. The authors believe that molnupiravir meets these requirements and is a breakthrough COVID-19 treatment. [ABSTRACT FROM AUTHOR]

We have developed a new idea to synthesize a key intermediate molecule by utilizing deep eutectic solvent (DES) and ultrasound in a multistep reaction to ensure process cost-effectiveness. To confirm the stability of reagents with DES, electronic energies were calculated at the B3LYP/6-31+G(d,p) level of theory. DES stabilized the reagents mainly due to strong intermolecular hydrogen bonding. Key intermediate (3) and final compounds (4a–n) were synthesized in a higher yield of 95% and 80%–88%, respectively. Further, final compounds (4a–n) were assessed for their anti-inflammatory, analgesic, ulcerogenic, and lipid peroxidation. The compounds 4f, 4g, 4j, 4l, and 4m showed good anti-inflammatory activity, while 4f, 4i, and 4n exhibited very good analgesic activity as compared to the standard drug. The ulcerogenicity of selected compounds was far less than the indomethacin. The ligands had also shown a good docking score (4f = −6.859 kcal/mol and 4n = −7.077 kcal/mol) as compared to control indomethacin (−6.109 kcal/mol) against the target protein COX-2. These derivatives have the potential to block this enzyme and can be used as NSAID. The state-of-art DFT theory was used to validate the lipid peroxidation mechanism of the active compounds which was in good agreement with the variations of BDEs and IP of the tested compounds. [ABSTRACT FROM AUTHOR]

Pyrazoline is an important five membered nitrogen heterocycle, which has been extensively researched upon. The ring is quite stable and has inspired chemists to carry out various structural variations in the ring. This has propelled the development of distinct pyrazolines with an array of pharmacological activities viz. anti-inflammatory, analgesic, antimicrobial, anticancer, antidepressant etc. The review aims at highlighting this pharmacological diversity of pyrazolines. The review is a gist of latest work done describing the pharmacological aspects and potential of pyrazoline ring.