Synthesis and antitubulin activity of N 1-and N4-substituted 3, 5-dinitro sulfanilamides against African Trypanosomes and Leishmania

…, M Mollet, G Riccio, R Brun, KA Werbovetz

Index: Bhattacharya, Gautam; Herman, Johnathan; Delfin, Dawn; Salem, Manar M.; Barszcz, Todd; Mollet, Mike; Riccio, Guy; Brun, Reto; Werbovetz, Karl A. Journal of Medicinal Chemistry, 2004 , vol. 47, # 7 p. 1823 - 1832

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Citation Number: 53

Abstract

Thirty analogues of N 1-phenyl-3, 5-dinitro-N 4, N 4-di-n-propylsulfanilamide (GB-II-5, compound 3), a new antikinetoplastid antimitotic agent, have been synthesized and evaluated. The addition of simple functional groups to the N1 aromatic ring generally decreases antiparasitic and antimitotic potency, but placement of a dibutyl substituent at the N4 nitrogen to give N 1-phenyl-3, 5-dinitro-N 4, N 4-di-n-butylsulfanilamide (compound 35 ...