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Synthesis of brequinar analogue inhibitors of malaria parasite dihydroorotate dehydrogenase.

Abstract：

:A series of 2-phenyl quinoline-4-carboxylic acid derivatives related to brequinar, an inhibitor of human dihydroorotate dehydrogenase (DHODH), has been prepared and evaluated as inhibitors of DHODH from the malaria parasite Plasmodium falciparum. Brequinar was essentially inactive against PfDHODH (IC(50) 880 microM) whereas several members of the series inhibited PfDHODH. Unexpectedly, replacement of the carboxylic acid required for brequinar to inhibit hDHODH was not essential in the diisopropylamides that inhibited PfDHODH.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Boa AN,Canavan SP,Hirst PR,Ramsey C,Stead AM,McConkey GA

doi

10.1016/j.bmc.2005.01.017

subject

Has Abstract

pub_date

2005-03-15 00:00:00

pages

1945-67

issue

6

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(05)00026-X

journal_volume

13

pub_type

杂志文章

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