Antikinetoplastid antimitotic activity and metabolic stability of dinitroaniline sulfonamides and benzamides

…, DL Sackett, M Kaiser, R Brun, KA Werbovetz

Index: George, Tesmol G.; Johnsamuel, Jayaseharan; Delfin, Dawn A.; Yakovich, Adam; Mukherjee, Mitali; Phelps, Mitch A.; Dalton, James T.; Sackett, Dan L.; Kaiser, Marcel; Brun, Reto; Werbovetz, Karl A. Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 16 p. 5699 - 5710

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Citation Number: 26

Abstract

N1-Phenyl-3, 5-dinitro-N4, N4-di-n-propylsulfanilamide (1) and N1-phenyl-3, 5-dinitro-N4, N4-di-n-butylsulfanilamide (2) show potent in vitro antimitotic activity against kinetoplastid parasites but display poor in vivo activity. Seventeen new dinitroaniline sulfonamide and eleven new benzamide analogs of these leads are reported here. Nine of the sulfonamides display in vitro IC50 values under 500nM against African trypanosomes, and the most ...