Publication Type : Journal Article
Publisher : Anti-Infective Agents
Source : Anti-Infective Agents, Issue 1 (2015)
Url : http://www.eurekaselect.com/node/124405/article
Keywords : Analogues, Antitubercular Agents, Isatin, molecular hybridization, mycobacteria, thiazole.
Campus : Kochi
School : School of Pharmacy
Department : Pharmaceutical Chemistry & Analysis
Year : 2015
Abstract : A series of isatin imines incorporated with 4-sustituted phenyl 2-amino thiazole was synthesizedon the basis of molecular hybridization drug design principle. The structures of the derivativeswere confirmed by IR, 1HNMR and Mass analyses. The titled derivatives were screened againstM.tuberculosis strain H37RVusing alamar blue susceptibility test. Compound 3-{[4-(4-hydroxyphenyl)-1, 3-thiazol-2-yl] imino}-1, 3-dihydro-2H-indol-2-one (IIT2) was found to be mostactive with a MIC of 6.25µg/ml. Preclinical evaluation of the compounds was ascertained by in silicotoxicity and ADME parameters. It has been concluded that the hydrogen contributing groups present in the phenyl systemof the titled scaffold favours the activity ratio.
Cite this Research Publication : N. Joy and Bijo Mathew, “Molecular Hybridization and Preclinical Evaluation of Imines From Para-substituted 4-phenyl 2-amino Thiazole Incorporated with Isatin Analogues as Antitubercular Agents”, Anti-Infective Agents, 13 vol., no. 1, 2015.