Synthesis and antiprotozoal activity of dicationic m-terphenyl and 1, 3-dipyridylbenzene derivatives

…, T Pandharkar, SK Jones, KA Werbovetz…

Index: Patrick, Donald A.; Ismail, Mohamed A.; Arafa, Reem K.; Wenzler, Tanja; Zhu, Xiaohua; Pandharkar, Trupti; Jones, Susan Kilgore; Werbovetz, Karl A.; Brun, Reto; Boykin, David W.; Tidwell, Richard R. Journal of Medicinal Chemistry, 2013 , vol. 56, # 13 p. 5473 - 5494

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Citation Number: 15

Abstract

4, 4 ″-Diamidino-m-terphenyl (1) and 36 analogues were prepared and assayed in vitro against T rypanosoma brucei rhodesiense, Trypanosoma cruzi, Plasmodium falciparum, and Leishmania amazonensis. Twenty-three compounds were highly active against T. b. rhodesiense or P. falciparum. Most noteworthy were amidines 1, 10, and 11 with IC50 of 4 nM against T. b. rhodesiense, and dimethyltetrahydropyrimidinyl analogues 4 and 9 with ...