| Literature DB >> 27298002 |
Hassan M Faidallah1, Siva S Panda2, Juan C Serrano3, Adel S Girgis4, Khalid A Khan1, Khalid A Alamry1, Tanya Therathanakorn3, Marvin J Meyers5, Francis M Sverdrup5, Christopher S Eickhoff5, Stephen G Getchell3, Alan R Katritzky3.
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.Entities:
Keywords: Antimalarial; Click chemistry; QSAR; Quinine; Triazole
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Year: 2016 PMID： 27298002 DOI： 10.1016/j.bmc.2016.05.060
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641