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Evaluation of furofuran as a P2 ligand for symmetry-based HIV protease inhibitors

✍ Scribed by Xiaoqi Chen; Lin Li; Dale J. Kempf; Hing Sham; Norman E. Wideburg; Ayda Saldivar; Sudthida Vasavanonda; Kennan C. Marsh; Edith McDonald; Daniel W. Norbeck

Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 313 KB
Volume: 6
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(96)00528-8

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✦ Synopsis

The hexahydrofurofuranyloxy group was evaluated as a conformationally constrained P2 ligand for symmetry-based HIV protease inhibitors. A number of compounds showed nM level activity against HIV in MT4 cells and lower protein binding than the licensed protease inhibitor ritonavir. However, replacement of 5-thiazole of ritonavir with a furofuran caused a reduction of the bioavailability in vivo.

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