4-羟基-5-吡咯啉酮-3-甲酰胺类HIV-1整合酶抑制剂。
4-Hydroxy-5-pyrrolinone-3-carboxamide HIV-1 integrase inhibitors.
作者信息
Pace Paola, Spieser Stéphane A H, Summa Vincenzo
机构信息
Department of Medicinal Chemistry, IRBM-MRL Rome, Via Pontina Km 30,600, 00040 Pomezia, Rome, Italy.
出版信息
Bioorg Med Chem Lett. 2008 Jul 15;18(14):3865-9. doi: 10.1016/j.bmcl.2008.06.056. Epub 2008 Jun 20.
PMID:18595690
Abstract
The viral enzyme integrase is essential for the replication of HIV-1 and, after the discovery of Isentress, represents a validated target for anti-retroviral therapy. Incorporation of the dihydroxycarbonyl pharmacophore into a pyrrolinone scaffold led to the discovery of 5-pyrrolinone-3-carboxamides as a structurally diverse class of HIV-1 integrase inhibitors.
摘要
病毒酶整合酶对于HIV-1的复制至关重要，在Isentress被发现后，它成为了抗逆转录病毒疗法的一个经过验证的靶点。将二羟基羰基药效团引入吡咯烷酮支架中，从而发现了5-吡咯烷酮-3-羧酰胺类化合物，这是一类结构多样的HIV-1整合酶抑制剂。
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