Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity

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• 作者：Alicia Regueiro-Ren ; Zheng Liu ; Yan Chen ; Ny Sin ; Sing-Yuen Sit ; Jacob J. Swidorski ; Jie Chen ; Brian L. Venables ; Juliang Zhu ; Beata Nowicka-Sans ; Tricia Protack ; Zeyu Lin ; Brian Terry ; Himadri Samanta ; Sharon Zhang ; Zhufang Li ; Brett R. Beno ; Xiaohua S. Huang ; Sandhya Rahematpura ; Dawn D. Parker ; Roy Haskell ; Susan Jenkins ; Kenneth S. Santone ; Mark I. Cockett ; Mark Krystal ; Nicholas A. Meanwell ; Umesh Hanumegowda ; Ira B. Dicker
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：June 9, 2016
• 年：2016
• 卷：7
• 期：6
• 页码：568-572
• 全文大小：313K
• 年卷期：0
• ISSN：1948-5875

文摘

HIV-1 maturation inhibition (MI) has been clinically validated as an approach to the control of HIV-1 infection. However, identifying an MI with both broad polymorphic spectrum coverage and good oral exposure has been challenging. Herein, we describe the design, synthesis, and preclinical characterization of a potent, orally active, second generation HIV-1 MI, BMS-955176 (2), which is currently in Phase IIb clinical trials as part of a combination antiretroviral regimen.