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Bioorg Med Chem. 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.

Author information

1
Department of Chemistry, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia.
2
Department of Chemistry & Physics, Augusta University, Augusta, GA 30912, USA. Electronic address: sspanda12@gmail.com.
3
Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, USA.
4
Pesticide Chemistry Department, National Research Centre, Dokki, Giza 12622, Egypt.
5
Center for World Health & Medicine, Saint Louis University, Saint Louis, MO 63104, USA.

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

PMID:
27298002
DOI:
10.1016/j.bmc.2016.05.060
[Indexed for MEDLINE]

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