Synthesis and antiprotozoal activities of dicationic bis (phenoxymethyl) benzenes, bis (phenoxymethyl) naphthalenes, and bis (benzyloxy) naphthalenes

…, T Wenzler, T Barzcz, KA Werbovetz, R Brun…

Index: Patrick, Donald A.; Bakunov, Stanislav A.; Bakunova, Svetlana M.; Suresh Kumar; Chen, Heidi; Jones, Susan Kilgore; Wenzler, Tanja; Barzcz, Todd; Werbovetz, Karl A.; Brun, Reto; Tidwell, Richard R. European Journal of Medicinal Chemistry, 2009 , vol. 44, # 9 p. 3543 - 3551

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Citation Number: 19

Abstract

A series of 37 dicationically substituted bis (phenoxymethyl) benzene bis (phenoxymethyl) naphthalene, and bis (benzyloxy) naphthalene analogues of pentamidine was prepared and evaluated for antiprotozoal activities and cytotoxicity in in vitro. 1, 3-Bis (4- amidinophenoxymethyl) benzene (1) was the most active against Trypanosoma brucei rhodesiense (IC50= 2.1 nM). 1, 3-Bis [4-(N-isopropylamidino) phenoxymethyl] benzene (2 ...