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Combinatorial synthesis of CCR5 antagonists.

Abstract：

:Herein we report the preparation of a combinatorial library of compounds with potent CCR5 binding affinity. The library design was aided by SAR generated in a traditional medicinal chemistry effort. Compounds with novel combinations of subunits were discovered that have high binding affinity for the CCR5 receptor. A potent CCR5 antagonist from the library, compound 11 was found to have moderate anti-HIV-1 activity.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Willoughby CA,Berk SC,Rosauer KG,Degrado S,Chapman KT,Gould SL,Springer MS,Malkowitz L,Schleif WA,Hazuda D,Miller M,Kessler J,Danzeisen R,Holmes K,Lineberger J,Carella A,Carver G,Emini EA

doi

10.1016/s0960-894x(01)00652-7

subject

Has Abstract

pub_date

2001-12-17 00:00:00

pages

3137-41

issue

24

eissn

0960-894X

issn

1464-3405

pii

S0960894X01006527

journal_volume

11

pub_type

杂志文章

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