Design, synthesis, characterization and antitubercular activity of some nov-el 2, 4-disubstituted thiazole derivatives

  • Gobala Krishnan P Research Scholar, JNTUA, Anantapuramu - 515002 Andhra Pradesh, India
  • Gnanaprakash K Department of Pharmaceutical Chemistry, Saastra College of Pharmaceutical Education and Research, Nellore – 524 311, Andhra Pradesh, India
  • Chandrasekhar KB Department of Chemistry, JNTUA, Anantapuramu - 515002 Andhra Pradesh, India

Abstract

Literature reviews reveal that thiazole and pyrazine carboxamide derivatives exhibit anticonvulsant, antimicrobial, anticancer and anti-tubercular activities due to the presence of –S-C=N- and-CO–NH- moiety. A series of thiazolyl pyrazine carboxamide derivatives (5a-j) were synthesized by condensation reaction between 2-amino, 4-substituted phenyl 2-amino thiazole and pyrazine 2-carboxylic acid. These synthesized thiazole derivatives (5a-j) were evaluated for their inhibitory activity against Mycobacterium tuberculosis (Mtb), H37Rv using microplate Alamar Blue assay (MABA). The compound, 5c and 5h showed high anti-mycobacterial activity with MIC value of 6.25 µg/ml, and the compound 5g also exhibited anti-mycobacterial activity with MIC value of 12.50 µg/ml. Molecular docking studies of these synthesized molecules with b-Ketoacyl-ACP Synthase (KasA) protein of Mycobacterium tuberculosis (Mtb) have been carried out to understand the mechanism of anti-mycobacterial action.

Keywords: 2-aminothiazole, Pyrazine 2-carboxylic acid, Mycobacterium tuber-culosis (Mtb), b-Ketoacyl-ACP Syn-thase (KasA), Antimycobacterial ac-tion

Downloads

Download data is not yet available.
Published
2019-04-23
Citations
How to Cite
Gobala Krishnan P, Gnanaprakash K, & Chandrasekhar KB. (2019). Design, synthesis, characterization and antitubercular activity of some nov-el 2, 4-disubstituted thiazole derivatives. International Journal of Research in Pharmaceutical Sciences, 10(2), 1504-1509. https://doi.org/10.26452/ijrps.v10i2.729
Section
Original Articles
Article Level Metrix
Abstract Views: 52
PDF Downloaded: 65