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Review
. 2016 Aug 15;24(16):3527-39.
doi: 10.1016/j.bmc.2016.05.060. Epub 2016 May 30.

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

Hassan M Faidallah  1 , Siva S Panda  2 , Juan C Serrano  3 , Adel S Girgis  4 , Khalid A Khan  1 , Khalid A Alamry  1 , Tanya Therathanakorn  3 , Marvin J Meyers  5 , Francis M Sverdrup  5 , Christopher S Eickhoff  5 , Stephen G Getchell  3 , Alan R Katritzky  3
Affiliations
Review

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

Hassan M Faidallah et al. Bioorg Med Chem. .

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.

Keywords: Antimalarial; Click chemistry; QSAR; Quinine; Triazole.

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