title: 5-Nitrothiazolylthiosemicarbazones: synthesis and antimycobacterial evaluation against tubercular and non-tubercular mycobacterial species.
abstract: Nineteen 5-nitrothiazolylthiosemicarbazones were synthesized from 5-nitrothiazole by three-step synthesis and evaluated for in vitro activities against seven mycobacterial species. Among them, N-(5-nitro-1, 3-thiazol-2-yl)-2-((Z)-4-[(phenylmethyl)oxy]phenylmethylidene)hydrazine-1-carbothioamide (4m) was found to be the most active compound with a minimum inhibitory concentration (MIC) of 0.23 microM against Mycobacterium tuberculosis H37 Rv, and was three times more potent than isoniazid and equally active as rifampicin. Compound 4m also inhibited six non-tubercular mycobacteria with MICs ranging from 1.88 to 30.25 microM.
authors.affiliation: Medicinal Chemistry and Antimycobacterial Research Laboratory, Pharmacy Group, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Hyderabad, Andhra Pradesh, India. dsriram@bits-hyderabad.ac.in
authors.forename: Dhrmarajan
authors.initials: D
authors.lastname: Sriram
authors.forename: Perumal
authors.initials: P
authors.lastname: Yogeeswari
authors.forename: Palaniappan
authors.initials: P
authors.lastname: Senthilkumar
authors.forename: Dewakar
authors.initials: D
authors.lastname: Sangaraju
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects*; D013045:Species Specificity; D013882:Thiosemicarbazones / Q000138:chemical synthesis* / Q000494:pharmacology*; D014709:Vero Cells
chemical_list: D000995:Antitubercular Agents; D013882:Thiosemicarbazones