Novel small molecule bradykinin B1 receptor antagonists. Part 3: hydroxyurea derivatives.

Abstract:

:Hydroxy urea moieties are introduced as a new class of bradykinin B(1) receptor antagonists. First, the SAR of the lead compound was systematically explored. Subsequent optimization resulted in the identification of several biaryl-based hydroxyurea bradykinin B(1) receptor antagonists with low-nanomolar activity and very high oral bioavailability in the rat.

journal_name

Bioorg Med Chem Lett

authors

Schnatbaum K,Schaudt M,Stragies R,Pfeifer JR,Gibson C,Locardi E,Scharn D,Richter U,Kalkhof H,Dinkel K,Zischinsky G

doi

10.1016/j.bmcl.2009.11.121

subject

Has Abstract

pub_date

2010-02-01 00:00:00

pages

1233-6

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)01691-6

journal_volume

20

pub_type

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