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Synthesis, biological evaluation, and docking studies of N-substituted acetamidines as selective inhibitors of inducible nitric oxide synthase.

Abstract：

:New acetamidines structurally related to N-(3-(aminomethyl)benzyl)acetamidine (1, W1400) were designed as inhibitors of inducible nitric oxide synthase (iNOS). Six compounds were found to be selective for iNOS over endothelial nitric oxide synthase (eNOS), and among them, the most active and selective compound was the N-benzylacetamidine 2. A docking study was also performed to shed light on the effects of the structural modifications on the interaction of the designed inhibitors with the NOS.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Maccallini C,Patruno A,Besker N,Alì JI,Ammazzalorso A,De Filippis B,Franceschelli S,Giampietro L,Pesce M,Reale M,Tricca ML,Re N,Felaco M,Amoroso R

doi

10.1021/jm800846u

subject

Has Abstract

pub_date

2009-03-12 00:00:00

pages

1481-5

issue

5

eissn

0022-2623

issn

1520-4804

pii

10.1021/jm800846u

journal_volume

52

pub_type

杂志文章

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