达芦那韦，一种从概念上来说全新的用于治疗耐药性艾滋病毒的HIV-1蛋白酶抑制剂。
Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV.
作者信息
Ghosh Arun K, Dawson Zachary L, Mitsuya Hiroaki
机构信息
Departments of Chemistry and Medicinal Chemistry, Purdue University, West Lafayette, IN 47907, USA.
出版信息
Bioorg Med Chem. 2007 Dec 15;15(24):7576-80. doi: 10.1016/j.bmc.2007.09.010. Epub 2007 Sep 14.
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.
摘要
我们基于结构的设计策略专门针对HIV-1蛋白酶主链，产生了许多极具效力的非肽类抑制剂。其中一种抑制剂，地瑞那韦（TMC114），含有一种基于结构设计的、具有高亲和力的P2配体，即3(R),3a(S),6a(R)-双四氢呋喃基脲（双四氢呋喃）。地瑞那韦最近已被批准用于治疗携带对先前现有的高效抗逆转录病毒疗法（HAART）方案无反应的多药耐药HIV-1变体的艾滋病患者。
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