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Synthesis and evaluation of novel triazolyl quinoline derivatives as potential antileishmanial agents. 2018

Akanksha Upadhyay, and Pragati Kushwaha, and Sampa Gupta, and Ranga Prasad Dodda, and Karthik Ramalingam, and Ruchir Kant, and Neena Goyal, and Koneni V Sashidhara
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram extension, Sitapur Road, Lucknow, 226031, India.

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.

UI MeSH Term Description Entries
D007893 Leishmania donovani A parasitic hemoflagellate of the subgenus Leishmania leishmania that infects man and animals and causes visceral leishmaniasis (LEISHMANIASIS, VISCERAL). The sandfly genera Phlebotomus and Lutzomyia are the vectors. Leishmania (Leishmania) donovani,Leishmania leishmania donovani,Leishmania donovanus,Leishmania leishmania donovanus,donovani, Leishmania leishmania,donovanus, Leishmania,donovanus, Leishmania leishmania,leishmania donovanus, Leishmania
D011804 Quinolines
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D000981 Antiprotozoal Agents Substances that are destructive to protozoans. Schizonticides,Agents, Antiprotozoal
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D015394 Molecular Structure The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds. Structure, Molecular,Molecular Structures,Structures, Molecular
D021261 Parasitic Sensitivity Tests Tests that demonstrate the relative effectiveness of chemotherapeutic agents against specific parasites. Drug Sensitivity Tests, Helminth,Drug Sensitivity Tests, Parasitic,Drug Sensitivity Tests, Protozoal,Helminth Drug Sensitivity Tests,Parasite Sensitivity Tests,Protozoa Drug Sensitivity Tests,Protozoal Drug Sensitivity Tests,Parasite Sensitivity Test,Parasitic Sensitivity Test,Sensitivity Test, Parasite,Sensitivity Test, Parasitic,Sensitivity Tests, Parasite,Test, Parasite Sensitivity,Test, Parasitic Sensitivity,Tests, Parasite Sensitivity,Tests, Parasitic Sensitivity

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