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Combinatorial synthesis of CCR5 antagonists

descriptionPublicationkeyboard_double_arrow_right Article 01 Dec 2001Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 11, pages 3,137-3,141 (issn: 0960-894X,

Authors: Lorraine Malkowitz; Scott C. Berk; Renee Danzeisen; Joseph Kessler; Michael W. Miller; Emilio A. Emini; William A. Schleif; +11 Authors

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

pmid: 11720860

Combinatorial synthesis of CCR5 antagonists

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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.

Related Organizations

United States Military Academy
United States
Merck & Co.
United States

Keywords

Structure-Activity Relationship, CCR5 Receptor Antagonists, HIV-1, Combinatorial Chemistry Techniques

1 Research products, page 1 of 1

BindingDB Entry 50011484: Combinatorial synthesis of CCR5 antagonists.
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