Discovery of BMS-955176, a Second Generation HIV-1 Maturation Inhibitor with Broad Spectrum Antiviral Activity
- 22 April 2016
- journal article
- research article
- Published by American Chemical Society (ACS) in ACS Medicinal Chemistry Letters
- Vol. 7 (6), 568-572
- https://doi.org/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
This publication has 16 references indexed in Scilit:
- Inhibitors of HIV-1 maturation: Development of structure–activity relationship for C-28 amides based on C-3 benzoic acid-modified triterpenoidsBioorganic & Medicinal Chemistry Letters, 2016
- C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1 maturation inhibitorsBioorganic & Medicinal Chemistry, 2016
- Alkyl Amine Bevirimat Derivatives Are Potent and Broadly Active HIV-1 Maturation InhibitorsAntimicrobial Agents and Chemotherapy, 2016
- HIV-1 assembly, release and maturationNature Reviews Microbiology, 2015
- Antiretroviral TherapyInfectious Disease Clinics of North America, 2014
- New Betulinic Acid Derivatives for Bevirimat-Resistant Human Immunodeficiency Virus Type-1Journal of Medicinal Chemistry, 2013
- Can the further clinical development of bevirimat be justified?AIDS, 2010
- Phase I and II Study of the Safety, Virologic Effect, and Pharmacokinetics/Pharmacodynamics of Single-Dose 3-O-(3′,3′-Dimethylsuccinyl)Betulinic Acid (Bevirimat) against Human Immunodeficiency Virus InfectionAntimicrobial Agents and Chemotherapy, 2007
- Remote Modulation of Amine Basicity by a Phenylsulfone and a Phenylthio GroupChemMedChem, 2007
- Drug evaluation: bevirimat--HIV Gag protein and viral maturation inhibitor.2006