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

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

  • ACS Med Chem Lett. 2016 Apr 22;7(6):568-72. doi: 10.1021/acsmedchemlett.6b00010.
Alicia Regueiro-Ren 1,  Zheng Liu 1,  Yan Chen 1,  Ny Sin 1,  Sing-Yuen Sit 1,  Jacob J Swidorski 1,  Jie Chen 1,  Brian L Venables 1,  Juliang Zhu 1,  Beata Nowicka-Sans 1,  Tricia Protack 1,  Zeyu Lin 1,  Brian Terry 1,  Himadri Samanta 1,  Sharon Zhang 1,  Zhufang Li 1,  Brett R Beno 1,  Xiaohua S Huang 1,  Sandhya Rahematpura 1,  Dawn D Parker 1,  Roy Haskell 1,  Susan Jenkins 1,  Kenneth S Santone 1,  Mark I Cockett 1,  Mark Krystal 1,  Nicholas A Meanwell 1,  Umesh Hanumegowda 1,  Ira B Dicker 1
Affiliations

Affiliation

  • 1 Departments of Discovery Chemistry, Chemical Synthesis, Virology, Computer-Assisted Drug Design, and Pharmaceutical Candidate Optimization, B ristol-Myers Squibb Research and Development , 5 Research Parkway, Wallingford, Connecticut 06492, United States.
PMID: 27326328 DOI: 10.1021/acsmedchemlett.6b00010
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.

Keywords

BMS-955176; HIV-1; antiviral; betulinic acid; maturation inhibitors; triterpene.

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