|
|||||
|
|
Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV |
|
| Authors: | Ghosh Arun K Dawson Zachary L Mitsuya Hiroaki |
| Affiliation: | aDepartments of Chemistry and Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA bDepartment of Hematology and Infectious Diseases, Kumamoto University School of Medicine, Kumamoto 860-8556, Japan cExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, Bethesda, MD 20892, USA |
| Abstract: | Our structure-based design strategies which specifically target the HIV-1 protease backbone, resulted in a number of exceedingly potent nonpeptidyl inhibitors. One of these inhibitors, darunavir (TMC114), contains a privileged, structure-based designed high-affinity P2 ligand, 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane (bis-THF). Darunavir has recently been approved for the treatment of HIV/AIDS patients harboring multidrug-resistant HIV-1 variants that do not respond to previously existing HAART regimens. |
| Keywords: | Protease inhibitors Darunavir Design and synthesis |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |