Synthesis, antimalarial properties and 2D-QSAR studies of novel triazole-quinine conjugates

Siva S Panda

doi:10.1016/j.bmc.2016.05.060

Synthesis, antimalarial properties and 2D-QSAR studies of novel triazole-quinine conjugates

Siva S Panda

Chemistry and Biochemistry

Research output: Contribution to journal › Article › peer-review

48 Scopus citations

Abstract

Click chemistry technique led to novel 1,2,3-triazole-quinine conjugates 8a-g, 10a-o, 11a-h and 13 utilizing benzotriazole-mediated synthetic approach with excellent yields. Some of the synthesized analogs (11a, 11d-h) exhibited antimalarial properties against Plasmodium falciparum strain 3D7 with potency higher than that of quinine (standard reference used) through in vitro standard procedure bio-assay. Statistically significant BMLR-QSAR model describes the bio-properties, validates the observed biological observations and identifies the most important parameters governing bio-activity.

Original language	English (US)
Pages (from-to)	3527-39
Number of pages	13
Journal	Bioorganic and Medicinal Chemistry
Volume	24
Issue number	16
DOIs	https://doi.org/10.1016/j.bmc.2016.05.060
State	Published - Aug 15 2016

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Journal Article

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10.1016/j.bmc.2016.05.060

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abstract = "Click chemistry technique led to novel 1,2,3-triazole-quinine conjugates 8a-g, 10a-o, 11a-h and 13 utilizing benzotriazole-mediated synthetic approach with excellent yields. Some of the synthesized analogs (11a, 11d-h) exhibited antimalarial properties against Plasmodium falciparum strain 3D7 with potency higher than that of quinine (standard reference used) through in vitro standard procedure bio-assay. Statistically significant BMLR-QSAR model describes the bio-properties, validates the observed biological observations and identifies the most important parameters governing bio-activity.",

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AB - Click chemistry technique led to novel 1,2,3-triazole-quinine conjugates 8a-g, 10a-o, 11a-h and 13 utilizing benzotriazole-mediated synthetic approach with excellent yields. Some of the synthesized analogs (11a, 11d-h) exhibited antimalarial properties against Plasmodium falciparum strain 3D7 with potency higher than that of quinine (standard reference used) through in vitro standard procedure bio-assay. Statistically significant BMLR-QSAR model describes the bio-properties, validates the observed biological observations and identifies the most important parameters governing bio-activity.

KW - Journal Article

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DO - 10.1016/j.bmc.2016.05.060

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JO - Bioorganic and Medicinal Chemistry

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ER -

Synthesis, antimalarial properties and 2D-QSAR studies of novel triazole-quinine conjugates

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