Synthesis and antimicrobial study of novel heterocyclic compounds from hydroxybenzophenones

Eur J Med Chem. 2005 Nov;40(11):1156-62. doi: 10.1016/j.ejmech.2005.04.005. Epub 2005 Jun 1.

Abstract

The triazolothiadiazine analogues 6a-e were obtained via a multistep synthesis sequences beginning with the hydroxybenzophenones 1a-e. Hydroxybenzophenones on reaction with ethyl chloroacetate affords ethyl (2-aroylaryloxy)acetates 2a-e which on treatment with hydrazine hydrate yields 2-(2-aroylaryloxy)acetohydrazides 3a-e. Intramolecular cyclization of 3a-e with carbon disulfide affords 5-(2-aroylaryloxy)methyl-1,3,4-oxadiazole-2-(3H)thiones 4a-e, which on treatment with hydrazine hydrate yields 4-amino-5-(2-aroyl aryloxy)methyl-1,2,4-triazole-3-(2H)thiones 5a-e. Condensation of 5a-e with alpha-halocarbonyl compound results in 3-(2-aroylaryloxy)methyl-6-phenyl-1,2,4-triazolo[3,4-b][1,3,4] thiadiazine 6a-e analogues. The compounds 4a-e, 5a-e and 6a-e were tested against variety of fungal and bacterial strains in comparison to fluconazole and chloramphenicol, respectively.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / pharmacology
  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / pharmacology
  • Benzophenones / chemical synthesis*
  • Benzophenones / chemistry
  • Benzophenones / pharmacology
  • Heterocyclic Compounds / chemical synthesis*
  • Heterocyclic Compounds / pharmacology
  • Microbial Sensitivity Tests
  • Oxadiazoles / chemical synthesis
  • Oxadiazoles / chemistry
  • Thiadiazines / chemical synthesis
  • Thiadiazines / chemistry

Substances

  • Anti-Infective Agents
  • Antifungal Agents
  • Benzophenones
  • Heterocyclic Compounds
  • Oxadiazoles
  • Thiadiazines
  • benzophenone