New HIV-1 reverse transcriptase inhibitors based on a tricyclic benzothiophene scaffold: synthesis, resolution, and inhibitory activity.
作者信息
Krajewski Krzysztof, Zhang Yijun, Parrish Damon, Deschamps Jeffrey, Roller Peter P, Pathak Vinay K
机构信息
Laboratory of Medicinal Chemistry, CCR, NCI-Frederick, NIH, Frederick, MD 21702, USA.
出版信息
Bioorg Med Chem Lett. 2006 Jun 1;16(11):3034-8. doi: 10.1016/j.bmcl.2006.02.049. Epub 2006 Mar 9.
PMID:16527484
Abstract
We synthesized, separated into enantiomers, and tested for the HIV-1 reverse transcriptase inhibitory activity a group of analogs of dimethyl-1-(1-piperidynyl)cyclobuta[b][1]benzothiophene-2,2a(7bH)-dicarboxylate (NSC-380292). Absolute configurations of the enantiomers were determined based on absolute X-ray structures and analysis of CD spectra. Within pairs of enantiomers the (R,R)-enantiomer was always much more potent HIV-1 reverse transcriptase inhibitor.
摘要
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