Showing papers in "Bioorganic & Medicinal Chemistry Letters in 2021"

TL;DR: Pyridones have been utilized as privileged scaffolds in drug discovery as discussed by the authors, where they serve both as a hydrogen bond acceptor and/or a donor, and act as a bioisostere for amides, phenyls, pyridines, and other nitrogen- or oxygen-containing heterocycles.

TL;DR: The activity results has emphasized the compounds 8k and 8l as potential leads for further development of antibacterial, anti-Candida, and anti-biofilm agents.

TL;DR: In this paper, a review summarizes these advances and provides perspective on future directions of antibacterial agents, including new compounds of known classes and new compounds with new mechanisms, and summarizes the recent advances in the antibacterial area.

TL;DR: In this paper, a new series of bis-1,2,3- and 1-2,4-triazoles (10a-m) were designed and efficiently synthesized using methyl salicylate as potential antimicrobial agents.

TL;DR: In this article, a class of structurally unique para-aminobenzenesulfonyl oxadiazoles as new potential antimicrobial agents was designed and synthesized from acetanilide.

TL;DR: In this paper, a series of novel 1,2,3-triazole based imidazole derivatives (3a-e) have been synthesized using spectroscopic techniques.

TL;DR: In this paper, the interaction of SARS-CoV-2 protein (A and B chains of nsp13) with different recently synthesized phenolic compounds (Sreenivasulu et al., Synthetic Communications, 2020, 112-122) has been investigated by using molecular docking, quantum chemical and molecular dynamics simulations methods.

TL;DR: Quinolin-3-yl-methyl-1,2,3-triazolyl-1.4H-ones 8j-v was synthesized by click chemistry as an ultimate tactic where [3+2] cycloaddition of azides with terminal alkynes has been evolved as discussed by the authors.

TL;DR: It is identified that cyclic sulfonamide derivatives are a promising new template for the development of anti-SARS-CoV-2 agents and have good safety profiles in hERG and cytotoxicity studies.

TL;DR: In this article, an aminopyrazole-based proteolysis targeting chimera (PROTAC 2) was proposed to selectively degrades cyclin-dependent kinase 9 (CDK9) in MiaPaCa2 cells and sensitiz them to Venetoclax mediated growth inhibition.

TL;DR: In this paper, a series of triazole-sulfonamide bearing pyrimidine derivatives were designed and synthesized via click chemistry and tested as inhibitors of human carbonic anhydrase (hCA) isoforms, such as hCA I, II, IX and XII, using a stopped flow CO2 hydrase assay.

TL;DR: In this paper, the authors identified four 1,2,4-triazole derivatives that inhibit FAK kinase significantly and evaluated their therapeutic potential, including 3c and 3d.

TL;DR: In this paper, the SARS-CoV-2 main protease (Mpro) showed no inhibitory activity at concentrations as high as 100μM and only a long linear peptide covering residues P6 to P5′ showed moderate inhibition.

TL;DR: The newly synthesized compounds 7a-j were evaluated for anti-inflammatory and analgesic action and most of them exerted comparable activity to the reference compound celecoxib and showed less ulcerogenic effect than the reference drug.

TL;DR: In this article, the authors highlight the latest progress in the discovery and development of safe and efficacious SMs to treat autoimmune and inflammatory diseases with each part representing a class of SMs, namely: protein kinases, nucleic acid-sensing pathways, and soluble ligands and receptors on cell surfaces.

TL;DR: The test results showed that these sesamol derivatives had a good antioxidant activity, among them, compound 4d had the best antioxidant activity.

TL;DR: In this paper, the biological activity detection methods of tubulin polymerization inhibitors are reviewed and a theoretical basis for the further study and selection of methods for tubulin inhibitors is provided.

TL;DR: In this paper, the authors developed isatin-derived azoles as new potential antimicrobial agents and showed that isatin hybridized 1,2,4-triazole 7a exhibited excellent inhibitory activity against E. coli.

TL;DR: A series of podophyllotoxin-naphthoquinone compounds 5a-p were synthesized in good yields using microwave assisted four-component reactions of 2-hydroxy-1,4 naphthoequinone, aromatic benzaldehydes, tetronic acid and ammonium acetate as discussed by the authors.

TL;DR: In this article, a series of naringenin derivatives were designed and synthesized as multifunctional anti-Alzheimer's disease (AD) agents, and the results showed that these derivatives displayed moderate-to-good acetylcholinesterase (AChE) and butyrylcholine choline (BuChE), inhibitory activities at the micromolar range (IC50, 12.91-62.52μm for AChE and 0.094-13.72-μM for BuChE).

TL;DR: In this article, a library of 23 pyrazole linked phenylthiazole compounds were synthesized, followed by screening for antimicrobial activity against five bacterial species and two fungi, and the most active compound 14b showed promising antibacterial activity against the Gram-positive methicillin-resistant Staphylococcus aureus (MRSA, ATCC 43300) strain (MIC 4μg/mL).

TL;DR: In this article, the synthesis and antifungal activity of hybrids of thiazolo[4,5-d]pyrimidines with (1H-1,2,4)triazoles are presented.

TL;DR: A Ta2O5-anchored piperidine-4-carboxylic acid (PPCA) nanoparticle has been synthesized and characterized in this paper, which is then used as a highly effective nanocatalyst for the synthesis of quinolin-2(1H)-one derivatives through CO bond functionalization.

TL;DR: In this paper, a head-to-head comparison of fifteen reported peptidomimetic inhibitors in a standard FRET-based SARS-CoV-2 3CLpro inhibition assay was conducted to compare and identify potent inhibitors for development.

TL;DR: In this paper, the synthesis of mesalamine and coumarin linked together by a diazo group was reported, and the potential of the synthesized compound was investigated through acetic acid induced ulcerative colitis in rat model.

TL;DR: A series of novel oxazolidinone derivatives with nitrogen-containing fused heterocyclic moiety with potent activity against Gram-positive pathogens comparable to Linezolid and Radezolid exhibited significant antibacterial activity and might be a promising drug candidate for further investigation.

TL;DR: Ten thiazole-based thiazolidinone hybrids bearing a 6-trifluoromethoxy substituent on the benzothiazole core were synthesized and evaluated against a panel of four bacterial strains Salmonellatyphimurium, Staphylococcusaureus, Escherichia coli and Listeriamonocytogenes and three resistant strains Pseudomonas aeruginosa, E.coli and MRSA.

TL;DR: In this paper, a nucleoside triphosphate analog bearing two simultaneous modifications at the level of the sugar (LNA) and the backbone (thiophosphate) was synthesized for enzymatic DNA synthesis.

TL;DR: Detailed optimization of the C2 triazole substituent identified 4-pyridyl as the preferred replacement for the carboxamide of MK-5204, leading to improvements in antifungal activity in the presence of serum, and increased oral exposure.

TL;DR: In this article, a three-component reaction sequence comprising Cu(I)-catalyzed 1,3-dipolar cycloaddition (CuAAC) followed by Cu-catalysed arylation of resulting 1,2,3triazole in the presence of ionic liquid [Emim]BF4 under microwave conditions involving.