title: Development of 5-nitrothiazole derivatives: identification of leads against both replicative and latent Mycobacterium tuberculosis.
abstract: Twenty eight 5-nitrothiazole derivatives were synthesized and evaluated for in vitro activities against Mycobacterium tuberculosis (MTB), cytotoxicity against HEK 293T. Among the compounds, 5-nitro-N-(5-nitrothiazol-2-yl)furan-2-carboxamide (20) was found to be the most active compound in vitro with MICs of 5.48 μM against log-phase culture of MTB and also non-toxic up to 100 μM.
authors.affiliation: Antitubercular Drug Discovery Laboratory, Department of Pharmacy, Birla Institute of Technology& Science - Pilani, Hyderabad Campus, Jawahar Nagar, Hyderabad 500 078, India.
authors.forename: Variam Ullas
authors.initials: VU
authors.lastname: Jeankumar
authors.forename: Manoj
authors.initials: M
authors.lastname: Chandran
authors.forename: Ganesh
authors.initials: G
authors.lastname: Samala
authors.forename: Mallika
authors.initials: M
authors.lastname: Alvala
authors.forename: Pulla Venkat
authors.initials: PV
authors.lastname: Koushik
authors.forename: Perumal
authors.initials: P
authors.lastname: Yogeeswari
authors.forename: Elena G
authors.initials: EG
authors.lastname: Salina
authors.forename: Dharmarajan
authors.initials: D
authors.lastname: Sriram
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D057809:HEK293 Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: C581042:5-nitrothiazole; D000900:Anti-Bacterial Agents; D013844:Thiazoles