Antiprotozoal activity of dicationic 3, 5-diphenylisoxazoles, their prodrugs and aza-analogues

…, SA Bakunov, SM Bakunova, T Wenzler, R Brun…

Index: Patrick, Donald A.; Bakunov, Stanislav A.; Bakunova, Svetlana M.; Wenzler, Tanja; Brun, Reto; Tidwell, Richard R. Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 1 p. 559 - 576

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Citation Number: 5

Abstract

Abstract Fifty novel prodrugs and aza-analogues of 3, 5-bis (4-amidinophenyl) isoxazole and its derivatives were prepared. Eighteen of the 24 aza-analogues exhibited IC 50 values below 25 nM against Trypanosoma brucei rhodesiense or Plasmodium falciparum. Six compounds had antitrypanosomal IC 50 values below 10 nM. Twelve analogues showed similar antiplasmodial activities, including three with sub-nanomolar potencies. Forty-four ...