FACILE TiCl<sub>4</sub>-CATALYZED SYNTHESIS OF NOVEL 1,2,4-TRIAZOLES APPENDED TO THIAZOLES

Authors

  • T. Gireesh PG Department of Studies in Chemistry, Karnatak University
  • R. R. Kamble PG Department of Studies in Chemistry, Karnatak University
  • R. K. Hunnur PG Department of Studies in Chemistry, Karnatak University
  • T. Taj PG Department of Studies in Chemistry, Karnatak University
  • M. Y. Kariduraganavar PG Department of Studies in Chemistry, Karnatak University

DOI:

https://doi.org/10.1007/1490

Keywords:

mesoionic compounds, sydnones, TiCl4, 1, 3-dipolar cycloaddition

Abstract

The reaction of sydnone-derived 3-aryl-5-methyl-1,3,4-oxadiazol-2(3H)-ones with thiourea and α-bromoacetophenone derivatives in the presence of a catalytic amount of TiCl4 produces 2-aryl-4-(4-aryl-1,3-thiazol-2-yl)-5-methyl-2,4-dihydro-3H-1,2,4-triazol-3-ones. The title compounds were screened for their antibacterial and antifungal activity. The toxicity of the compounds was evaluated in terms of mutagenicity, tumorigenicity, and reproductive effects. The drug-relevant properties (ClogP, druglikeness, and drug score) were calculated, and the structure–activity relationship was discussed.

Also published in Chemistry of Heterocyclic Compounds, 2011, 47 (7), pp 877-885

http://link.springer.com/article/10.1007/s10593-011-0849-2

Downloads

Published

2014-01-17

Issue

No. 7 (2011)

Section

Original Papers