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Antikinetoplastid antimitotic activity and metabolic stability of dinitroaniline sulfonamides and benzamides.

Abstract：

:N(1)-Phenyl-3,5-dinitro-N(4),N(4)-di-n-propylsulfanilamide (1) and N(1)-phenyl-3,5-dinitro-N(4),N(4)-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 IC(50) values under 500 nM against African trypanosomes, and the most active antikinetoplastid compounds also inhibit the in vitro assembly of purified leishmanial tubulin with potencies similar to that of 2. While several of the potent compounds are rapidly degraded by rat liver S9 fractions in vitro, N(1)-(3-hydroxy)phenyl-3,5-dinitro-N(4),N(4)-di-n-butylsulfanilamide (21) displays an IC(50) value of 260 nM against African trypanosomes in vitro and is more stable than 2 in the in vitro metabolism assay.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

George TG,Johnsamuel J,Delfín DA,Yakovich A,Mukherjee M,Phelps MA,Dalton JT,Sackett DL,Kaiser M,Brun R,Werbovetz KA

doi

10.1016/j.bmc.2006.04.017

subject

Has Abstract

pub_date

2006-08-15 00:00:00

pages

5699-710

issue

16

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(06)00299-9

journal_volume

14

pub_type

杂志文章

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