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  • Title: Triazino indole-quinoline hybrid: a novel approach to antileishmanial agents.
    Author: Sharma R, Pandey AK, Shivahare R, Srivastava K, Gupta S, Chauhan PM.
    Journal: Bioorg Med Chem Lett; 2014 Jan 01; 24(1):298-301. PubMed ID: 24314395.
    Abstract:
    A novel series of 1,2,4-triazino-[5,6b]indole-3-thione covalently linked to 7-chloro-4-aminoquinoline have been synthesized and evaluated for their in vitro activity against extracellular promastigote and intracellular amastigote form of Leishmania donovani. Among all tested compounds, compounds 7a and 7b were found to be the most active with IC50 values 1.11, 0.36μM and selectivity index (SI) values 67, >1111, respectively, against amastigote form of L. donovani which is several folds more potent than the standard drugs, miltefosine (IC50=8.10μM, SI=7) and sodium stibo-gluconate (IC50=54.60μM, SI⩾7).
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