Abstract

SYNTHESIS, CHARACTERIZATION, IN VITRO AND IN SLICO STUDIES OF SOME NOVEL SUBSTITUTED 1,3,4-OXADIAZOLE-3(2H)-YL-ETHANONE DERIVATIVES

Anitha Huliyurdurga Channigarayappa, Sreenivasa Swamy*, Mohan R. Nadigar, Vivek Chandramohan and Shivaraja Govindaiaha

ABSTRACT

This work involves synthesis of novel 1,3,4-oxadiazole-3(2H)-yl)ethanone derivatives via dehydrative cyclization of acyl hydrozones in moderate to good yields, starting from chalcones. The dehydrative C–O coupling was achieved under metal-free conditions by using propylphosphonic anhydride (T3P®) a proficient reagent for one-pot transformation and acetic anhydride as dehydratent. Structures of the synthesized molecules were supported by FT-IR, 1H NMR, 13C NMR, Mass spectral and CHN elemental analysis. Synthesized oxadiazole derivatives were evaluated for their biological properties. In Silico study was done in an effort to understand the structural interaction of oxadiazoles with target proteins. The outcomes of the present study specify that dehydrative cyclization of the acyl hydrozones into novel 1,3,4-oxadiazole nucleus lead to the discovery of potent antimicrobial, anthelmintic and anti-inflammatory agents with a significant importance.

Keywords: Antimicrobial, Anthelmintic, Anti-inflammatory, Dehydrosqualene synthase, Molecular modeling, and 1,3,4-Oxadiazoles.