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

2016; American Chemical Society; Volume: 7; Issue: 6 Linguagem: Inglês

10.1021/acsmedchemlett.6b00010

1948-5875

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 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,

HIV/AIDS Research and Interventions

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.