Synthesis, antiplatelet and in silico evaluations of novel N-substituted-phenylamino-5-methyl-1H-1,2,3-triazole-4-carbohydrazides

  • Bioorg Med Chem. 2009 May 15;17(10):3713-9. doi: 10.1016/j.bmc.2009.03.053.
Alessandro K Jordão  1 ,  Vitor F Ferreira ,  Emerson S Lima ,  Maria C B V de Souza ,  Eduardo C L Carlos ,  Helena C Castro ,  Reinaldo B Geraldo ,  Carlos R Rodrigues ,  Maria C B Almeida ,  Anna C Cunha
Affiliations
  • 1. Universidade Federal Fluminense, Departamento de Química Orgânica, Outeiro de São João Batista, s/n degrees , Niterói, 24020-141 Rio de Janeiro, Brazil.
PMID: 19380229 DOI: 10.1016/j.bmc.2009.03.053
Abstract

This paper describes the synthesis, antiplatelet and theoretical evaluations of 10 N-substituted-phenylamino-5-methyl-1H-1,2,3-triazole-4-carbohydrazides (2a-j). These compounds were synthesized, characterized and screened for their in vitro antiplatelet profile against human platelet aggregation using arachidonic acid, adrenaline and ADP as agonists. Among NAH derivatives 2a-j, the compounds 2a, 2c, 2e, 2g and 2h were the most promising molecules with significant antiplatelet activity.