Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1367952 | Bioorganic & Medicinal Chemistry Letters | 2005 | 4 Pages |
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
Authors
Carmen Abate, Renata Kolanos, Malgorzata Dukat, Vince Setola, Bryan L. Roth, Richard A. Glennon,