Journal ArticleDOI
Oxazolidinones as Anti-tubercular Agents: Discovery, Development and Future Perspectives
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TLDR
The usefulness of these oxazolidinones in the drug resistant TB is already established and Toxicity, especially myelosuppression, has been an important limiting factor for their development.Abstract:
TB drug development pipeline represents varied structural classes of molecules. Oxazolidinones represent synthetic anti-bacterial agents with unique mechanism of action having wide spectrum of activity, oral bioavailability and well established SAR. They act by inhibiting translation at the initiation phase of protein synthesis. Linezolid was the first oxazolidinone to reach the market in the year 2000 for the treatment of methicillin-resistant staphylococcal and vancomycin-resistant enterococcal infections. Oxazolidinones have shown very good anti-mycobacterial activities. Several oxazolidinones are currently in development for their possible use in TB therapy. Oxazolidinones are classified on the basis of C-ring modifications. DuP-721 was the first oxazolidinone having good anti-TB activity. Linezolid, sutezolid and AZD5847 are in clinical development. Several other C-ring modifications have shown promising results. The usefulness of these oxazolidinones in the drug resistant TB is already established. Toxicity, especially myelosuppression, has been an important limiting factor for their development.read more
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Journal ArticleDOI
An overview of new antitubercular drugs, drug candidates, and their targets
Aparna Bahuguna,Diwan S. Rawat +1 more
TL;DR: Recent progress in the discovery of newly developed and Food and Drug Administration approved drugs as well as repurposed drugs, their targets, mode of action, drug‐target interactions, and their structure‐activity relationship are discussed.
Journal ArticleDOI
A straightforward one-pot synthesis of bioactive N-aryl oxazolidin-2-ones via a highly efficient Fe3O4@SiO2-supported acetate-based butylimidazolium ionic liquid nanocatalyst under metal- and solvent-free conditions
TL;DR: The synthesized nanocomposite proves its supremacy as an environmentally benign catalyst in the reaction of aniline and its derivatives with ethylene carbonate to form bioactive N-aryl oxazolidin-2-ones under metal-, ligand-, and solvent-free conditions.
Journal ArticleDOI
Nanostructured lipid carriers for incorporation of copper(II) complexes to be used against Mycobacterium tuberculosis.
Mariana Rillo Sato,João Augusto Oshiro Junior,Rachel Temperani Amaral Machado,Paula Carolina de Souza,Débora L. Campos,Fernando Rogério Pavan,Patrícia Bento da Silva,Marlus Chorilli +7 more
TL;DR: The results suggest that NLCs may be a powerful tool to optimize the activity of copper(II) complexes against M. tuberculosis.
Journal ArticleDOI
Benzo[d]thiazole-2-carbanilides as new anti-TB chemotypes: Design, synthesis, biological evaluation, and structure-activity relationship.
Tejas M. Dhameliya,Rishu Tiwari,Arkaprabha Banerjee,Sahaj Pancholia,Dharmarajan Sriram,Dulal Panda,Asit K. Chakraborti +6 more
TL;DR: Molecular docking suggests that the compounds 7w, 4i and 4n bind to the catalytic site of the enzyme ATP Phosphoribosyltransferase (HisG) and might be attributed to their anti-TB potential.
Journal ArticleDOI
Efficient Access to Chiral 2-Oxazolidinones via Ni-Catalyzed Asymmetric Hydrogenation: Scope Study, Mechanistic Explanation, and Origin of Enantioselectivity
Yuanhua Liu,Zhiyuan Yi,Xuanliang Yang,Heng Wang,Congcong Yin,Minyan Wang,Xiu-Qin Dong,Xumu Zhang,Xumu Zhang +8 more
TL;DR: Cheap transition metal Ni-catalyzed asymmetric hydrogenation of 2-oxazolones was successfully developed in this article, which provided an efficient synthetic strategy to prepare various chiral 2oxazolidinones.
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