|
|||||
|
|
Spiropiperidine CCR5 antagonists |
|
| Authors: | David M Rotstein Stephen D Gabriel Ferenc Makra Lubov Filonova Shelley Gleason Christine Brotherton-Pleiss Lina Q Setti Alejandra Trejo-Martin Eun Kyung Lee Surya Sankuratri Changhua Ji Andre deRosier Marianna Dioszegi Gabrielle Heilek Andreas Jekle Pamela Berry Paul Weller Cheng-I Mau |
| Institution: | aRoche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA |
| Abstract: | A novel series of CCR5 antagonists has been identified, utilizing leads from high-throughput screening which were further modified based on insights from competitor molecules. Lead optimization was pursued by balancing opposing trends of metabolic stability and potency. Selective and potent analogs with good pharmacokinetic properties were successfully developed. |
| Keywords: | CCR5 antagonist Chemokine Anti-HIV-1 Antiviral Spiropiperidine |
| 本文献已被 ScienceDirect 等数据库收录！ | |