Synthesis and evaluation of novel indolylthiadiazinoazetidinones and indolylthiadiazinothiazolidinones as antimicrobial agents

Arch Pharm (Weinheim). 2010 Feb;343(2):98-107. doi: 10.1002/ardp.200900203.

Abstract

Some new 5-methoxy/ethoxy-2,3-[2'-(3''-chloro-2''-oxo-4''-substituted-aryl-1''-azetidinyl)-1',3',4'-thiadiazino]indoles 13-20 and 5-methoxy/ethoxy-2,3-[2'-(2''-substituted-aryl-4''-oxo-1'',3''-thiazolidin-3''-yl)-1',3',4'-thiadiazino]indoles 21-28 have been synthesized from 5-methoxy/ethoxy-2,3-[2'-(substituted-benzylidinylimino)-1',3',4'-thiadiazino]indoles 5-12. These newly synthesized compounds were characterized by elemental and spectral analysis. Further, compounds 5-28 of the present series have been screened for their antibacterial and antifungal activities. Both minimal inhibitory concentration (MIC) and inhibition zones were determined in order to monitor the efficacy of the synthesized compounds. Compounds 14 and 16 were found to be the most potent members of the present series, they showed maximal antibacterial and antifungal properties much better than the standard drugs.

Publication types

  • Comparative Study

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Azetidines / chemical synthesis
  • Azetidines / chemistry
  • Azetidines / pharmacology*
  • Microbial Sensitivity Tests
  • Structure-Activity Relationship
  • Thiadiazines / chemical synthesis
  • Thiadiazines / chemistry
  • Thiadiazines / pharmacology
  • Thiazolidines / chemical synthesis
  • Thiazolidines / chemistry
  • Thiazolidines / pharmacology*

Substances

  • Anti-Bacterial Agents
  • Antifungal Agents
  • Azetidines
  • Thiadiazines
  • Thiazolidines