Article ID Journal Published Year Pages File Type
1367952 Bioorganic & Medicinal Chemistry Letters 2005 4 Pages PDF
Abstract

Optically active pyrrolidinylmethylindole analogs related in structure to the benzenesulfonyltryptamine 5-HT6 receptor antagonist MS-245 were evaluated and their R-isomers were found to bind with affinity higher than their S-enantiomers.

Graphical abstractChiral analogs of the 5-HT6 ligand MS-245 (Ki ca. 2 nM) were examined; for example, 5d (Ki = 0.3 nM) binds with higher affinity than its S-enantiomer (Ki = 1.7 nM), and with 30 times greater affinity than its counterpart lacking the benzenesulfonyl group.Figure optionsDownload full-size imageDownload as PowerPoint slide

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Physical Sciences and Engineering Chemistry Organic Chemistry
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