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  • Title: Synthesis and evaluation of novel triazolyl quinoline derivatives as potential antileishmanial agents.
    Author: Upadhyay A, Kushwaha P, Gupta S, Dodda RP, Ramalingam K, Kant R, Goyal N, Sashidhara KV.
    Journal: Eur J Med Chem; 2018 Jun 25; 154():172-181. PubMed ID: 29793211.
    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.
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