Structure-function analysis of antimicrotubule dinitroanilines against promastigotes of the parasitic protozoan Leishmania mexicana

Author:

Chan M M1,Tzeng J1,Emge T J1,Ho C T1,Fong D1

Affiliation:

1. Department of Biological Sciences, State University of New Jersey, Piscataway 08855.

Abstract

Although leishmaniasis is a major tropical disease, the currently available drugs are toxic and inadequate. We show that the antimicrotubule herbicide trifluralin has antileishmania activity. The present study aimed at deducing the relationship between the structure of the molecule and its antiprotozoan activity. Nine dinitroanilines, all of which were analogs of trifluralin, were compared. We found that pendimethalin was 2.5-fold more potent than trifluralin, and the higher efficacy may be correlated with molecular structural features that increase the accessibility to one nitro group. This association was further supported by molecular modeling. Moreover, trifluralin samples from two sources differed in their activities by more than threefold, and gas column chromatography showed that impurities were present in the more potent sample.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Reference34 articles.

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2. Drugs with colchicine-like effects that specifically disassemble plant but not animal microtubules;Bajer A. S.;Ann. N. Y. Acad. Sci.,1986

3. The herbicide trifluralin is active against microtubule-based oral morphogenesis in Stentor coeruleus;Banerjee S.;Cytobios,1975

4. Chan M. M. and D. Fong. 1989. Identification of a microtubule drug which differentially inhibits leishmania but not mammalian cell growth. J. Cell. Biochem. 13E:130.

5. Inhibition of leishmanias but not host macrophages by the antitubulin herbicide trifluralin;Chan M. M.;Science,1990

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