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Design, Synthesis, and Testing of Antiprotozoal Activity of Primin and Analogues

Journal: Journal of Medicinal and Chemical Sciences (Vol.2, No. 4)

Publication Date:

Authors : ; ; ; ; ;

Page : 140-143

Keywords : 1) Antiprotozoal activities; 2) Natural product-derived compounds; 3)Quinones; 4) C-H functionalization; 5)NMR spectroscopy;

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Abstract

A set of conformationally restricted analogues of the natural product primin were synthesized as potential antiprotozoal agents. The synthesis utilizes quinone C-H functionalization methods to enable an efficient and easy access to primin analogues. The antiprotozoal activities of this series were evaluated in a panel of parasites and compared with the natural product primin. For all synthesized primin analogues a potent in vitro activity was found against the pathogen Trypanosoma brucei rhodesiense (IC50 < 0.05 µg/mL). The observed antiprotozoal activity is not related to production of reactive oxygen species (ROS). Initial results of the in vivo experiments with a T. b. rhodesiense rodent animal model of the human disease were also reported. Intraperitoneal injection administration of compound 7 resulted in complete clearance of T. b. rhodesiense in tested rodent animals 24 hours after the last treatment. Our results show that the primin scaffold represents a new scaffold for further development of potent inhibitors of Trypanosoma brucei rhodesiense.

Last modified: 2019-03-24 21:16:35