Dataset Information

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

ABSTRACT: 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.

SUBMITTER: Regueiro-Ren A

PROVIDER: S-EPMC4904268 | biostudies-literature | 2016 Jun

REPOSITORIES: biostudies-literature

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

Regueiro-Ren Alicia A Liu Zheng Z Chen Yan Y Sin Ny N Sit Sing-Yuen SY Swidorski Jacob J JJ Chen Jie J Venables Brian L BL Zhu Juliang J Nowicka-Sans Beata B Protack Tricia T Lin Zeyu Z Terry Brian B Samanta Himadri H Zhang Sharon S Li Zhufang Z Beno Brett R BR Huang Xiaohua S XS Rahematpura Sandhya S Parker Dawn D DD Haskell Roy R Jenkins Susan S Santone Kenneth S KS Cockett Mark I MI Krystal Mark M Meanwell Nicholas A NA Hanumegowda Umesh U Dicker Ira B IB

ACS medicinal chemistry letters 20160422 6

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. ...[more]

PMID: 27326328

Dataset Information

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

Publications

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

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