1423045-83-3

Upstream product

• 1394157-97-1 C₄₈H₇₃NO₅ 
• 59868-82-5 3-O-acetylbetulinic acid chloride 
• 174740-43-3 9-[((1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-9-Hydroxy-1-isopropenyl-5a,5b,8,8,11a-pentamethyl-icosahydro-cyclopenta[a]chrysene-3a-carbonyl)-amino]-nonanoic acid 
• 10376-50-8 3-O-acetylbetulinic acid 
• 17347-61-4 2,2-dimethylsuccinic anhydride 
• 1394157-72-2 benzyl N-[N'-(betulinic acid-28-oyl)-9-aminononanoyl]-L-glutaminate 

Relevant academic research and scientific papers

New betulinic acid derivatives for bevirimat-resistant human immunodeficiency virus type-1

Bevirimat (1, BVM) is an anti-HIV agent that blocks HIV-1 replication by interfering with HIV-1 Gag-SP1 processing at a late stage of viral maturation. However, clinical trials of 1 have revealed a high baseline drug resistance that is attributed to naturally occurring polymorphisms in HIV-1 Gag. To overcome the drug resistance, 28 new derivatives of 1 were synthesized and tested against compound 1-resistant (BVM-R) HIV-1 variants. Among them, compound 6 exhibited much improved activity against several HIV-1 strains carrying BVM-R polymorphisms. Compound 6 was at least 20-fold more potent than 1 against the replication of NL4-3/V370A, which carries the most prevalent clinical BVM-R polymorphism in HIV-1 Gag-SP1. Thus, compound 6 merits further development as a potential anti-AIDS clinical trial candidate.