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

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13 Citations (Scopus)

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 languageEnglish (US)
Pages (from-to)3527-39
Number of pages13
JournalBioorganic and Medicinal Chemistry
Volume24
Issue number16
DOIs
StatePublished - Aug 15 2016

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Triazoles
Quinine
Quantitative Structure-Activity Relationship
Antimalarials
Click Chemistry
Bioassay
Plasmodium falciparum
Bioactivity
benzotriazole
In Vitro Techniques

Keywords

  • Journal Article

Cite this

Synthesis, antimalarial properties and 2D-QSAR studies of novel triazole-quinine conjugates. / Panda, Siva S.

In: Bioorganic and Medicinal Chemistry, Vol. 24, No. 16, 15.08.2016, p. 3527-39.

Research output: Contribution to journalArticle

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