Combinatorial synthesis of CCR5 antagonists.

Basic Information

ID: ALA1134148

Journal: Bioorg Med Chem Lett

Title: Combinatorial synthesis of CCR5 antagonists.

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.

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.

CiteXplore: 11720860

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

Patent ID: