2-(4-Phenyl-4-Piperidinyl)EthyI Amine-Based CCR5 Antagonists: Derivatizations at the N-terminal of the Piperidine Ring

摘要

Discovery of the chemokine receptor CCR5 as a co-receptor for HIV-1 infections revealed a novel approach to HJV-1 treatments and preventions. CCR5, a member from the family of 7TM G-protein coupled receptors, thus became an attractive target pursued in the pharmaceutical industry. With the recent successful developments of several small molecules in clinic, these CCR5 antagonists hold great promise to be the next generation of anti-HIV medicines. This poster will describe our efforts at the N-terminal piperidine ring of template A to improve pharmacological properties of derived molecules.