The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.

Abstract:

:The introduction of a functionalised amido substituent into a series of 1-(biphenylmethylacetamido)-pyrimidones has given a series of inhibitors of recombinant lipoprotein-associated phospholipase A(2) with sub-nanomolar potency and very encouraging developability properties. Diethylaminoethyl derivative 32, SB-435495, was selected for progression to man.

journal_name

Bioorg Med Chem Lett

authors

Blackie JA,Bloomer JC,Brown MJ,Cheng HY,Elliott RL,Hammond B,Hickey DM,Ife RJ,Leach CA,Lewis VA,Macphee CH,Milliner KJ,Moores KE,Pinto IL,Smith SA,Stansfield IG,Stanway SJ,Taylor MA,Theobald CJ,Whittaker CM

doi

10.1016/s0960-894x(02)00473-0

subject

Has Abstract

pub_date

2002-09-16 00:00:00

pages

2603-6

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960894X02004730

journal_volume

12

pub_type

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