2-(Alkyl/Aryl)Amino-6-Benzylpyrimidin-4(3H)-ones as Inhibitors of Wild-Type and Mutant HIV-1: Enantioselectivity Studies
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- 作者：Dante Rotili ; Alberta Samuele ; Domenico Tarantino ; Rino Ragno ; Ira Musmuca ; Flavio Ballante ; Giorgia Botta ; Ludovica Morera ; Marco Pierini ; Roberto Cirilli ; Maxim B. Nawrozkij ; Emmanuel Gonzalez ; Bonaventura Clotet ; Marino Artico ; Jos茅 A. Est茅 ; Giovanni Maga ; Antonello Mai
- 刊名：Journal of Medicinal Chemistry
- 出版年：2012
- 出版时间：April 12, 2012
- 年：2012
- 卷：55
- 期：7
- 页码：3558-3562
- 全文大小：236K
- 年卷期：v.55,no.7(April 12, 2012)
- ISSN：1520-4804
文摘
The single enantiomers of two pyrimidine-based HIV-1 non-nucleoside reverse transcriptase inhibitors, 1 (MC1501) and 2 (MC2082), were tested in both cellular and enzyme assays. In general, the R forms were more potent than their S counterparts and racemates and (R)-2 was more efficient than (R)-1 and the reference compounds, with some exceptions. Interestingly, (R)-2 displayed a faster binding to K103N RT with respect to WT RT, while (R)-1 showed the opposite behavior.