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2‐Mercaptoquinoline Analogues: A Potent Antileishmanial Agent
Author(s) -
Koley Suvajit,
Tiwari Neeraj,
Singh Rakesh Kumar,
Singh Maya Shankar
Publication year - 2018
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201703095
Subject(s) - amastigote , cytotoxicity , leishmania , intracellular , leishmania donovani , chemistry , leishmaniasis , ic50 , biochemistry , pharmacology , biology , in vitro , parasite hosting , visceral leishmaniasis , immunology , world wide web , computer science
Leishmaniases are endemic in various countries and parasite is developing resistance against available drugs. Thus, development of new drugs against Leishmania is an open area of investigation for synthetic organic chemist. In order to meet this challenge, a series of 2‐mercaptoquinoline derivatives have been synthesized and docked into the active site of Trypanothione reductase (TryR) enzyme required for redox balance of parasite. These were screened on promastigote and intracellular amastigote stages of L. donovani and found to show high levels of antileishmanial activity together with no cytotoxicity. Some of the synthesized compounds tested here, exhibited very steady and promising leishmanicidal activity against both promastigotes & intracellular amastigotes form, and the observations have been superbly supported by the docking results.