1. Synthesis and Evaluation of Novel 2,2-Dimethylthiochromanones as Anti-Leishmanial Agents.
- Author
-
Coll S, Alhazmi M, de Aguiar Amaral P, Bourgeade-Delmas S, Le Lamer AC, and Barlow JW
- Subjects
- Animals, Antiprotozoal Agents chemistry, Biological Products chemistry, Biological Products pharmacology, Cell Line, Chromones chemistry, Mice, Parasitic Sensitivity Tests, Antiprotozoal Agents chemical synthesis, Antiprotozoal Agents pharmacology, Chromones chemical synthesis, Chromones pharmacology, Leishmania drug effects
- Abstract
Within this work, we describe the design and synthesis of a range of novel thiochromanones based on natural products reported to possess anti-leishmanial action, and their synthetic derivatives. All compounds were elaborated via the key intermediate 2,2,6-trimethoxythiochromanone, which was modified at the benzylic position to afford various ester, amine and amide analogues, substituted by chains of varying lipophilicity. Upon testing in Leishmania , IC
50 values revealed the most potent compounds to be phenylalkenyl and haloalkyl amides 11a and 11e , with IC50 values of 10.5 and 7.2 μM, respectively.- Published
- 2021
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