Literature DB >> 29793211

Synthesis and evaluation of novel triazolyl quinoline derivatives as potential antileishmanial agents.

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.
Copyright © 2018 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Leishmaniasis; Pharmacophore hybridization; Triazolyl 2-methyl-4-phenylquinoline-3-carboxylate

Mesh:

Substances:

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


  6 in total

1.  Anti-Leishmanial and Cytotoxic Activities of a Series of Maleimides: Synthesis, Biological Evaluation and Structure-Activity Relationship.

Authors:  Yongxian Fan; Yuele Lu; Xiaolong Chen; Babu Tekwani; Xing-Cong Li; Yinchu Shen
Journal:  Molecules       Date:  2018-11-05       Impact factor: 4.411

Review 2.  1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview.

Authors:  Khurshed Bozorov; Jiangyu Zhao; Haji A Aisa
Journal:  Bioorg Med Chem       Date:  2019-07-04       Impact factor: 3.641

3.  Systematic in silico Evaluation of Leishmania spp. Proteomes for Drug Discovery.

Authors:  Crhisllane Rafaele Dos Santos Vasconcelos; Antonio Mauro Rezende
Journal:  Front Chem       Date:  2021-04-27       Impact factor: 5.221

Review 4.  The Potential of 2-Substituted Quinolines as Antileishmanial Drug Candidates.

Authors:  Philippe M Loiseau; Kaluvu Balaraman; Gillian Barratt; Sébastien Pomel; Rémy Durand; Frédéric Frézard; Bruno Figadère
Journal:  Molecules       Date:  2022-04-02       Impact factor: 4.411

Review 5.  Recent advances in the synthesis of biologically and pharmaceutically active quinoline and its analogues: a review.

Authors:  Abdanne Weyesa; Endale Mulugeta
Journal:  RSC Adv       Date:  2020-06-02       Impact factor: 4.036

Review 6.  Quinoline derivatives volunteering against antimicrobial resistance: rational approaches, design strategies, structure activity relationship and mechanistic insights.

Authors:  Nitish Kumar; Aanchal Khanna; Komalpreet Kaur; Harmandeep Kaur; Anchal Sharma; Preet Mohinder Singh Bedi
Journal:  Mol Divers       Date:  2022-10-05       Impact factor: 3.364

  6 in total

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