Design, Synthesis, and X-ray Crystallographic Analysis of a Novel Class of HIV-1 Protease Inhibitors

• Published in: Journal of medicinal chemistry Vol. 54; no. 20; pp. 7176 - 7183
• Main Authors: Ganguly, Ashit K, Alluri, Sesha S, Caroccia, Danielle, Biswas, Dipshikha, Wang, Chih-Hung, Kang, Eunhee, Zhang, Yong, McPhail, Andrew T, Carroll, Steven S, Burlein, Christine, Munshi, Vandna, Orth, Peter, Strickland, Corey
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 27.10.2011; Amer Chemical Soc
• Subjects: Carbamates - chemical synthesis; Carbamates - chemistry; Chemistry, Medicinal; Crystallography, X-Ray; Drug Design; HIV Protease - chemistry; HIV Protease Inhibitors - chemical synthesis; HIV Protease Inhibitors - chemistry; Life Sciences & Biomedicine; Models, Molecular; Molecular Structure; Pharmacology & Pharmacy; Protein Binding; Protein Conformation; Science & Technology; Stereoisomerism; Structure-Activity Relationship; Thiazepines - chemical synthesis; Thiazepines - chemistry; TMC114; POTENT; GENERATION; DISCOVERY

In the present paper, design, synthesis, X-ray crystallographic analysis, and HIV-1 protease inhibitory activities of a novel class of compounds are disclosed. Compounds 28–30, 32, 35, and 40 were synthesized and found to be inhibitors of the HIV-1 protease. The crucial step in their synthesis invol...