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Synthesis and evaluation of 2-pyridyl pyrimidines with in vitro antiplasmodial and antileishmanial activity |
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| Authors: | Chitalu C Musonda Gavin A Whitlock Michael J Witty Reto Brun Marcel Kaiser |
| Institution: | 1. University of Cape Town, Department of Chemistry, P/B Rondebosch 7700, Cape Town, South Africa;2. Department of Chemistry, Pfizer Global R&D, Ramsgate Road, Sandwich, Kent CT13 9NJ, United Kingdom;3. Swiss Tropical Institute, Socinstrasse 57, CH-4002 Basel, Switzerland |
| Abstract: | A series of 2-pyridyl pyrimidines, reported inhibitors of Plasmodium falciparum methionine aminopeptidase 1b were synthesized and evaluated for their antiplasmodial activities. An analysis of physicochemical properties demonstrated a link between lipophilicity and antiparasitic activity. Cross screening of the library against cultured Leishmania donovani parasites revealed this class of compounds as potent inhibitors of parasite development in vitro. |
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