Author/Authors :
Christopher A. Willoughby، نويسنده , , Scott C. Berk، نويسنده , , Keith G. Rosauer، نويسنده , , Silvia Degrado، نويسنده , , Kevin T. Chapman، نويسنده , , Sandra L. Gould، نويسنده , , Martin S. Springer، نويسنده , , Lorraine Malkowitz، نويسنده , , William A. Schleif، نويسنده , , Daria Hazuda، نويسنده , , Michael Miller، نويسنده , , Joseph Kessler، نويسنده , , Renee Danzeisen، نويسنده , , Karen Holmes، نويسنده , , Janet Lineberger، نويسنده , , Anthony Carella، نويسنده , , Gwen Carver، نويسنده , , Emilio A. Emini، نويسنده ,
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.
