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.
Copyright (c) 2009. Published by Elsevier Masson SAS.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antiprotozoal Agents / chemical synthesis*
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Antiprotozoal Agents / chemistry
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Antiprotozoal Agents / pharmacology*
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Antiprotozoal Agents / toxicity
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Cell Line
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Cell Survival / drug effects
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Drug Evaluation, Preclinical
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Inhibitory Concentration 50
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Leishmania donovani / drug effects*
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Leishmania donovani / growth & development
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Life Cycle Stages
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Mice
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Pyrimidines / chemical synthesis*
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Pyrimidines / chemistry
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Pyrimidines / pharmacology*
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Pyrimidines / toxicity
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Triazines / chemical synthesis*
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Triazines / chemistry
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Triazines / pharmacology*
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Triazines / toxicity
Substances
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Antiprotozoal Agents
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Pyrimidines
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Triazines