Novel lead structures for antimalarial farnesyltransferase inhibitors

…, J Sakowski, J Wiesner, R Ortmann…

Index: Kettler; Sakowski; Wiesner; Ortmann; Jomaa; Schlitzer, Martin Pharmazie, 2005 , vol. 60, # 5 p. 323 - 327

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Citation Number: 13

Abstract

Through the combination of nitrophenylfurylacryloyl moiety which has been designed to occupy an aryl binding site of farnesyltransferase with several AA (X)-peptidomimetic substructures some novel farnesyltransferase inhibitors were obtained. Evaluation of their antimalarial activity and some initial modifications yielded a 4-benzophenone-and a sulfonamid-based novel lead for antimalarial farnesyltransferase inhibitors.