Vivian I. Bonano, Jenicer K. U. Yokoyama-Yasunaka, Danilo C. Miguel, Scott A. Jones, Jeffrey A. Dodge and Silvia R. B. Uliana Discovery of Synthetic Leishmania Inhibitors by Screening of a 2-Arylbenzothiophene Library Chemical Biology & Drug Design 83
The screening of an estrogen receptor modulator related library of compounds allowed the identification of benzothiophenes as a new scaffold with antileishmanial properties. Three compounds devoid of estrogen receptor interaction were identified with increased potency against the parasite. Structure-activity data for the synthetic benzothiophenes evaluated in this study indicates that optimal antileishmanial potency is dependent on the presence of two basic side chains.
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