One pot synthesis and biological activity evaluation of novel Schiff bases derived from 2-hydrazinyl-1,3,4-thiadiazole

Chem Pharm Bull (Tokyo). 2013;61(2):160-6. doi: 10.1248/cpb.c12-00651. Epub 2012 Nov 27.

Abstract

Considering the structural features of a group of known potent inhibitors of human platelet aggregation containing hydrazone structural backbone, a series of novel hydrazone derivatives of 2-hydrazinyl-1,3,4-thiadiazole were synthesized using a one-pot process and tested for their inhibitory activity against platelet aggregation induced by arachidonic acid and ADP. Among the derivatives, compounds 3l, 3o and 3p exhibited the highest antiplatelet aggregation activity. The derivatives were also screened for their potential antimycobacterial activity and compounds 3g, 3k, 3p and 3q were among the most active compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Diphosphate / chemistry
  • Adenosine Diphosphate / pharmacology
  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Arachidonic Acid / antagonists & inhibitors
  • Arachidonic Acid / pharmacology
  • Humans
  • Hydrazones / chemistry*
  • Microbial Sensitivity Tests
  • Mycobacterium bovis / drug effects
  • Platelet Aggregation / drug effects
  • Platelet Aggregation Inhibitors / chemical synthesis*
  • Platelet Aggregation Inhibitors / chemistry
  • Platelet Aggregation Inhibitors / pharmacology
  • Schiff Bases / chemical synthesis*
  • Schiff Bases / chemistry
  • Schiff Bases / pharmacology
  • Thiadiazoles / chemistry*

Substances

  • Anti-Bacterial Agents
  • Hydrazones
  • Platelet Aggregation Inhibitors
  • Schiff Bases
  • Thiadiazoles
  • 1,3,4-thiadiazole
  • Arachidonic Acid
  • Adenosine Diphosphate