Non-thiol farnesyltransferase inhibitors: N-(4-aminoacylamino-3-benzoylphenyl)-3-[5-(4-nitrophenyl)-2 furyl] acrylic acid amides and their antimalarial activity

…, J Wiesner, K Silber, P Haebel, R Ortmann…

Index: Kettler, Katja; Wiesner, Jochen; Silber, Katrin; Haebel, Peter; Ortmann, Regina; Sattler, Isabel; Dahse, Hans-Martin; Jomaa, Hassan; Klebe, Gerhard; Schlitzer, Martin European Journal of Medicinal Chemistry, 2005 , vol. 40, # 1 p. 93 - 101

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Citation Number: 25

Abstract

Water solubility was previously found to be essential for in vivo-antimalarial activity of a novel type of benzophenone-based farnesyltransferase inhibitors. Introduction of a α-amino group into the phenylacetic acid substructure provided more soluble compounds with high farnesyltransferase inhibitory activity. The in vitro-antimalarial activity was detrimentally influenced by this structural modification.