Combinatorial synthesis of CCR5 antagonists.


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.

Cite this paper

@article{Willoughby2001CombinatorialSO, title={Combinatorial synthesis of CCR5 antagonists.}, author={Christopher A Willoughby and Scott C Berk and Keith G Rosauer and Sylvia J Degrado and Kevin T Chapman and Sandra L Gould and Martin S. Springer and Lorraine Malkowitz and William A Schleif and Daria J. Hazuda and Michael D. Miller and Jason A Kessler and Renee C Danzeisen and Karen W. Holmes and Janet E. Lineberger and Alexandre Carella and Gwen Carver and Emilio A . Emini}, journal={Bioorganic & medicinal chemistry letters}, year={2001}, volume={11 24}, pages={3137-41} }