Synthesis and anti-microbial activity of isothiosemicarbazones and cyclic analogues

Farmaco. 2002 Oct;57(10):809-17. doi: 10.1016/s0014-827x(02)01288-0.

Abstract

It is known that some derivatives of both thiourea and thiosemicarbazide exhibit potent anti-microbial activity. In order to investigate the effects on the biological properties of structural modifications of such structures, we have synthesised and studied some arylidenisothiosemicarbazones. In this paper we report on the synthesis and structure-activity relationships of some isothiosemicarbazones, where the arylidene group has been replaced with a cycloalkyl group and the sulfur atom has been either differently substituted or enclosed in a thiazole ring.

MeSH terms

  • Animals
  • Anti-Bacterial Agents
  • Anti-Infective Agents / chemical synthesis
  • Anti-Infective Agents / pharmacology*
  • Chlorocebus aethiops
  • Fungi / drug effects
  • Gram-Positive Bacteria / drug effects
  • Hydrophobic and Hydrophilic Interactions
  • Microbial Sensitivity Tests
  • Spectrometry, Mass, Electrospray Ionization
  • Structure-Activity Relationship
  • Thiosemicarbazones / chemistry*
  • Thiosemicarbazones / pharmacology*
  • Vero Cells / drug effects

Substances

  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Thiosemicarbazones