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Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.

Abstract：

:Two closely related scaffolds were identified through an uHTS campaign as desirable starting points for the development of Rho-Kinase (ROCK) inhibitors. Here, we describe our hit-to-lead evaluation process which culminated in the rapid discovery of potent leads such as 22 which successfully demonstrated an early in vivo proof of concept for anti-hypertensive activity.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Wu F,Büttner FH,Chen R,Hickey E,Jakes S,Kaplita P,Kashem MA,Kerr S,Kugler S,Paw Z,Prokopowicz A,Shih CK,Snow R,Young E,Cywin CL

doi

10.1016/j.bmcl.2010.04.070

subject

Has Abstract

pub_date

2010-06-01 00:00:00

pages

3235-9

issue

11

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)00540-8

journal_volume

20

pub_type

杂志文章

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