Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV-1 Protease Inhibitors [electronic resource]

• Ngôn ngữ: eng
• Ký hiệu phân loại: 610 Medicine and health
• Thông tin xuất bản: Argonne, Ill. : Oak Ridge, Tenn. : Argonne National Laboratory ; Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy, 2017
• Mô tả vật lý: Size: p. 1292-1297 : , digital, PDF file.
• Bộ sưu tập: Metadata
• ID: 260373
• Chủ đề: 1. 60 applied life sciences; 2. Hiv-1 protease inhibitors; 3. Mk-8718; 4. Piperazine sulfonamide; 5. Pl-100

Tóm tắt

Using the HIV-1 protease binding mode of MK-8718 and PL-100 as inspiration, a novel aspartate binding bicyclic piperazine sulfonamide core was designed and synthesized. The resulting HIV-1 protease inhibitor containing this core demonstrated an 60-fold increase in enzyme binding affinity and a 10-fold increase in antiviral activity relative to MK-8718.