2. Academic Validation
  3. Triazino indole-quinoline hybrid: a novel approach to antileishmanial agents

Triazino indole-quinoline hybrid: a novel approach to antileishmanial agents

  • Bioorg Med Chem Lett. 2014 Jan 1;24(1):298-301. doi: 10.1016/j.bmcl.2013.11.018.
Rashmi Sharma 1,  Anand Kumar Pandey 1,  Rahul Shivahare 2,  Khushboo Srivastava 2,  Suman Gupta 2,  Prem M S Chauhan 3
Affiliations

Affiliations

  • 1 Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
  • 2 Division of Parasitology, CSIR-Central Drug Research Institute, Lucknow 226 031, India.
  • 3 Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India. Electronic address: prem_chauhan_2000@yahoo.com.
PMID: 24314395 DOI: 10.1016/j.bmcl.2013.11.018
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).

Keywords

Antileishmanial; Hybrid; In vitro; Leishmania donovani; Quinoline; Triazino-indole.

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