2. Academic Validation
  3. Synthesis and biological evaluation of new [1,2,4]triazino[5,6-b]indol-3-ylthio-1,3,5-triazines and [1,2,4]triazino[5,6-b]indol-3-ylthio-pyrimidines against Leishmania donovani

Synthesis and biological evaluation of new [1,2,4]triazino[5,6-b]indol-3-ylthio-1,3,5-triazines and [1,2,4]triazino[5,6-b]indol-3-ylthio-pyrimidines against Leishmania donovani

  • Eur J Med Chem. 2010 Jun;45(6):2359-65. doi: 10.1016/j.ejmech.2010.02.015.
Leena Gupta 1,  Naresh Sunduru,  Aditya Verma,  Saumya Srivastava,  Suman Gupta,  Neena Goyal,  Prem M S Chauhan
Affiliations

Affiliation

  • 1 Division of Medicinal and Process Chemistry, Central Drug Research Institute, MG Road, Lucknow 226001, U.P., India.
PMID: 20371140 DOI: 10.1016/j.ejmech.2010.02.015
Abstract

A series of [1,2,4]triazino[5,6-b]indol-3-ylthio-1,3,5-triazines and [1,2,4]triazino[5,6-b]indol-3-ylthio-pyrimidines were synthesized and screened for their in vitro antileishmanial activity against Leishmania donovani. Among all, 8 compounds have shown more than 90% inhibition against promastigotes and IC50 in the range of 4.01-57.78 microM against amastigotes. Compound 5, a triazino[5,6-b]indol-3-ylthio-1,3,5-triazine derivative was found to be the most active and least toxic with 20- & 10-fold more selectivity (S.I.=56.61) as compared to that of standard drugs pentamidine and sodium stibogluconate (SSG), respectively.

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