| Literature DB >> 29793211 |
Akanksha Upadhyay1, Pragati Kushwaha1, Sampa Gupta1, Ranga Prasad Dodda1, Karthik Ramalingam2, Ruchir Kant3, Neena Goyal4, Koneni V Sashidhara5.
Abstract
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 μM) and intracellular amastigotes (IC50 ranging from 7.06 to 34.9 μM) than the control, miltefosine (IC50 = 8.4 μM), with less cytotoxicity in comparison to the standard drugs. Overall results revealed that prototype signify a new structural lead for antileishmanial chemotherapy.Entities:
Keywords: Leishmaniasis; Pharmacophore hybridization; Triazolyl 2-methyl-4-phenylquinoline-3-carboxylate
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Year: 2018 PMID: 29793211 DOI: 10.1016/j.ejmech.2018.05.014
Source DB: PubMed Journal: Eur J Med Chem ISSN: 0223-5234 Impact factor: 6.514