Article
Design of gem-difluoro-bis-tetrahydrofuran as P2 ligand for HIV-1 protease inhibitors to improve brain penetration: synthesis, X-ray studies, and biological evaluation.
ChemMedChem - 1 Jan 2015
Ghosh Arun K, Yashchuk Sofiya, Mizuno Akira, Chakraborty Nilanjana, Agniswamy Johnson, Wang Yuan-Fang, Aoki Manabu, Gomez Pedro Miguel Salcedo, Amano Masayuki, Weber Irene T, Mitsuya Hiroaki
Abstract excerpt
The structure-based design, synthesis, biological evaluation, and X-ray structural studies of fluorine-containing HIV-1 protease inhibitors are described. The synthesis of both enantiomers of the gem-difluoro-bis-THF ligands was carried out in a stereoselective manner using a Reformatskii-Claisen reaction as the key step. Optically active ligands were converted into protease inhibitors. Two of these inhibitors,...
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