Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity
| Autor: | Sing-Yuen Sit, Ny Sin, Umesh Hanumegowda, Dawn D. Parker, Zheng Liu, Alicia Regueiro-Ren, Xiaohua S. Huang, Brian Lee Venables, Brian Terry, Brett R. Beno, Sharon Zhang, Ira B. Dicker, Roy Haskell, Jacob Swidorski, Zhufang Li, Mark I. Cockett, Beata Nowicka-Sans, Zeyu Lin, Nicholas A. Meanwell, Tricia Protack, Sandhya Rahematpura, Juliang Zhu, Susan Jenkins, Himadri Samanta, Mark Krystal, Yan Chen, Kenneth S. Santone, Jie Chen |
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| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Maturation inhibitor 030106 microbiology Organic Chemistry Human immunodeficiency virus (HIV) Pharmacology Biology medicine.disease_cause Biochemistry Clinical trial 03 medical and health sciences Regimen Broad spectrum 030104 developmental biology Orally active Drug Discovery medicine |
| Zdroj: | ACS Medicinal Chemistry Letters. 7:568-572 |
| ISSN: | 1948-5875 |
| DOI: | 10.1021/acsmedchemlett.6b00010 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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