Investigation on the Effects of Antimicrobial imidazo[2,1-b]thiazole Derivatives on the Genitourinary Microflora

Med Chem. 2018;14(3):311-319. doi: 10.2174/1573406413666171010110819.

Abstract

Background: Fused five-membered heterocyclic rings containing bridgehead nitrogen atom are particularly versatile in the field of medicinal chemistry because of their different biological activities. Among them, the imidazo[2,1-b]thiazole is an attractive fused heterocyclic core that has been extensively studied.

Objective: The aim of the current study was to study the therapeutic applications of imidazo[2,1- b]thiazole derivatives as antimicrobial agents for the treatment of genitourinary infections.

Method: A traditional synthetic methodology was involved to obtain a small series of imidazothiazole derivatives.

Results: Herein, we report the antimicrobial activity of the imidazo[2,1-b]thiazole or imidazo[2,1- b]thiazolidine derivatives against selected fungi, Gram-positive and Gram-negative bacteria. Moreover, experiments were carried out to investigate the interference towards the endogenous microbiota.

Conclusion: The most interesting of the series are the thiocyano derivatives (19, 23) showing a good profile for the treatment of genitourinary infections: a spectrum of activity covering both bacteria and fungi together with a reduced impact versus critical lines of Lactobacillus exerting defense against pathogens.

Keywords: imidazo[2, 1-b]thiazole; Ampicillin; antiproliferative effects; bifidobacteria; lactobacilli; urogenital pathogens.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / pharmacology*
  • Antifungal Agents / chemical synthesis
  • Antifungal Agents / pharmacology
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / pharmacology
  • Bifidobacterium / drug effects
  • Econazole / pharmacology
  • HeLa Cells
  • Humans
  • Imidazoles / chemical synthesis
  • Imidazoles / pharmacology*
  • Lactobacillus / drug effects
  • Microbial Sensitivity Tests
  • Thiazoles / chemical synthesis
  • Thiazoles / pharmacology*
  • Urogenital System / microbiology

Substances

  • Anti-Bacterial Agents
  • Antifungal Agents
  • Antineoplastic Agents
  • Imidazoles
  • Thiazoles
  • Econazole