Dayam Raveendra, Al-Mawsawi Laith Q, Neamati Nouri
Department of Pharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA 90089, USA.
Bioorg Med Chem Lett. 2007 Nov 15;17(22):6155-9. doi: 10.1016/j.bmcl.2007.09.061. Epub 2007 Sep 20.
The beta-diketoacid class of HIV-1 integrase (IN) inhibitors represent the first potent class of compounds specific for the strand transfer catalytic activity of the viral enzyme. Previously, utilizing a beta-diketoacid pharmacophore as a search query, we identified a substituted 2-pyrrolinone with modest IN inhibitory activity from a database of small-molecules [Dayam, R.; Sanchez, T.; Neamati, N. J. Med. Chem.2005, 48, 8009]. In efforts to optimize this class of IN inhibitors, we carried out a structure-activity relationship analysis around the 2-pyrrolinone core. Here, we present a new class of 2-pyrrolinone IN inhibitors.
HIV-1整合酶（IN）抑制剂中的β-二酮酸类代表了针对该病毒酶链转移催化活性的首批强效特异性化合物。此前，我们利用β-二酮酸药效团作为搜索查询词，从小分子数据库中鉴定出一种具有适度IN抑制活性的取代2-吡咯啉酮[Dayam, R.; Sanchez, T.; Neamati, N. J. Med. Chem.2005, 48, 8009]。为了优化这类IN抑制剂，我们围绕2-吡咯啉酮核心进行了构效关系分析。在此，我们展示了一类新型的2-吡咯啉酮IN抑制剂。
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