A new class of potential chloroquine-resistance reversal agents for Plasmodia: syntheses and biological evaluation of 1-(3'-diethylaminopropyl)-3-(substituted phenylmethylene)pyrrolidines.

Abstract:

:1-(3'-Diethylaminopropyl)-3-(substituted phenylmethylene)pyrrolidines were synthesized and evaluated for CQ-resistant reversal activity. In general the compounds of the series elicit better biological response than their phenylmethyl analogues. The most active compound 4b has been evaluated in vivo in detail, and the results are presented. The possible mode of action of the compounds of this series is by inhibition of the enzyme heme oxygenase, thereby increasing the levels of heme and hemozoin, which are lethal to the parasite.

journal_name

J Med Chem

authors

Batra S,Srivastava P,Roy K,Pandey VC,Bhaduri AP

doi

10.1021/jm000083u

keywords:

subject

Has Abstract

pub_date

2000-09-07 00:00:00

pages

3428-33

issue

18

eissn

0022-2623

issn

1520-4804

pii

jm000083u

journal_volume

43

pub_type

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