title: Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
abstract: In an effort to discover new anti-tubercular agents, a series of new diarylpyrrole-oxazolidinone conjugates have been designed and synthesized. The anti-tubercular activity of these new conjugates (4a-n and 5a-d) against Mycobacterium tuberculosis H37Rv and drug resistance strains such as M. tuberculosis Rif(R) and M. tuberculosis XDR are discussed, wherein compound 4i has been found to be the most potent amongst the series. MTT assay was performed on the active conjugates of the series (4b-f, 4i and 5c) against mouse macrophage (J-774) cells to evaluate cytotoxic effects and selective index values. In addition, these conjugates (4a-n and 5a-d) are also tested against a panel of Gram-positive and Gram-negative bacterial strains. The docking studies have been carried out to provide some insight into the mechanism of action for this class of compounds.
authors: Medicinal Chemistry and Pharmacology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India. ahmedkamal@iict.res.in
authors: Ahmed
authors: A
authors: Kamal
authors: P
authors: P
authors: Swapna
authors: Rajesh V C R N C
authors: RV
authors: Shetti
authors: Anver Basha
authors: AB
authors: Shaik
authors: M P
authors: MP
authors: Narasimha Rao
authors: Farheen
authors: F
authors: Sultana
authors: Inshad Ali
authors: IA
authors: Khan
authors: Sandeep
authors: S
authors: Sharma
authors: Nitin Pal
authors: NP
authors: Kalia
authors: Sunil
authors: S
authors: Kumar
authors: Bagul
authors: B
authors: Chandrakant
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D004305:Dose-Response Relationship, Drug; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D051379:Mice; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D023303:Oxazolidinones / Q000737:chemistry / Q000494:pharmacology*; D011758:Pyrroles / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D011758:Pyrroles