title: Synthesis and biological evaluation of substituted 4-arylthiazol-2-amino derivatives as potent growth inhibitors of replicating Mycobacterium tuberculosis H₃₇Rv.
abstract: In search of potential therapeutics for tuberculosis, we describe herein synthesis and biological evaluation of some substituted 4-arylthiazol-2-amino derivatives as modified analogues of the antiprotozoal drug Nitazoxanide (NTZ), which has recently been reported as potent inhibitor of Mtb H(37)Rv (Mtb MIC=52.12 μM) with an excellent ability to evade resistance. Among the synthesized derivatives, the two compounds 7a (MIC=15.28 μM) and 7c (MIC=17.03 μM) have exhibited about three times better Mtb growth inhibitory activity over NTZ and are free from any cytotoxicity (Vero CC(50) of 244 and 300 μM respectively). These two compounds represent promising leads for further optimization.
authors.affiliation: Division of Medicinal and Process Chemistry, Central Drug Research Institute, CSIR, Lucknow 226 001, India.
authors.forename: Kuldeep K
authors.initials: KK
authors.lastname: Roy
authors.forename: Supriya
authors.initials: S
authors.lastname: Singh
authors.forename: Sandeep K
authors.initials: SK
authors.lastname: Sharma
authors.forename: Ranjana
authors.initials: R
authors.lastname: Srivastava
authors.forename: Vinita
authors.initials: V
authors.lastname: Chaturvedi
authors.forename: Anil K
authors.initials: AK
authors.lastname: Saxena
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D004305:Dose-Response Relationship, Drug; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects* / Q000254:growth & development; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D013844:Thiazoles