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Novel 2-aminooctahydrocyclopentalene-3a-carboxamides as potent CCR2 antagonists.

Abstract：

:Novel CCR2 antagonists with a novel 2-aminooctahydrocyclopentalene-3a-carboxamide scaffold were designed. SAR studies led to a series of potent compounds. For example, compound 51 had a good PK profile in both dog and monkey, and exhibited excellent efficacy when dosed orally in an inflammation model in hCCR2 KI mice. In addition, an asymmetric synthesis to the core structures was developed.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Cai C,Kang FA,Hou C,O'Neill JC,Opas E,McKenney S,Johnson D,Sui Z

doi

10.1016/j.bmcl.2012.10.069

subject

Has Abstract

pub_date

2013-01-01 00:00:00

pages

351-4

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)01360-1

journal_volume

23

pub_type

杂志文章

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