期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 154, 期 -, 页码 172-181出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.05.014
关键词
Leishmaniasis; Pharmacophore hybridization; Triazolyl 2-methyl-4-phenylquinoline-3-carboxylate
资金
- CSIR-CDRI, Govt. of India
- Sophisticated Analytical Instrument Facility (SAIF) CDRI, Lucknow, India
- CSIR, New Delhi
The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover novel series of 25 compounds for the development of new antileishmanial agents. A series of triazolyl 2-methyl-4-phenylquinoline-3-carboxylate derivatives has been synthesized via click chemistry inspired molecular hybridization approach and evaluated against Leishmania donovani. Most of the screened derivatives exhibited significant in vitro anti-leishmanial activity against promastigote (IC50 ranging from 2.43 to 45.75 mu M) and intracellular amastigotes (IC50 ranging from 7.06 to 34.9 mu M) than the control, miltefosine (IC50 = 8.4 mu M), with less cytotoxicity in comparison to the standard drugs. Overall results revealed that prototype signify a new structural lead for antileishmanial chemotherapy. (C) 2018 Elsevier Masson SAS. All rights reserved.
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