Quantitative structure-activity relationships of 6-anilinouracils as inhibitors of Bacillus subtilis DNA polymerase III.

Abstract:

:Quantitative structure-activity relationships (QSAR) of a series of 6-anilinouracil derivatives were developed for their inhibitory activity against the wild-type DNA polymerase III (pol III) and a mutant enzyme, pol III/azp-12, derived from Bacillus subtilis. Interaction between inhibitors and both enzymes appears to result solely from hydrophobic binding. Comparison of the substituent contributions indicates increased hydrophobic character and a minor change of shape of the inhibitor binding site of the mutant enzyme. Because the two enzymes have identical Km values for substrates, the inhibitor binding site is thought to be distinct from the enzyme active site.

journal_name

J Med Chem

authors

Wright GE,Gambino JJ

doi

10.1021/jm00368a013

subject

Has Abstract

pub_date

1984-02-01 00:00:00

pages

181-5

issue

2

eissn

0022-2623

issn

1520-4804

journal_volume

27

pub_type

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