1‐Thia‐4, 7‐diaza‐spiro[4.4]nonane‐3, 6‐dione: A Structural Motif for 5‐hydroxytryptamine 6 Receptor Antagonism. (26th December 2013)

• Record Type: Journal Article
• Authors: Hostetler, Greg; Dunn, Derek; McKenna, Beth A.; Kopec, Karla; Chatterjee, Sankar
• Is Part Of: Chemical biology & drug design. Volume 83:Number 2(2014:Feb.)
• Page Start: 149
• Page End: 153
• Publication Date: 2013-12-26
• Subjects: Drugs -- Design -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; 615.19005
• DOI: 10.1111/cbdd.12240
• Languages: English
• ISSNs: 1747-0277

Abstract

<abstract abstract-type="main" id="cbdd12240-abs-0001"> <title> <x xml:space="preserve">Abstract</x> </title> <p>A series of potent 5‐hydroxytryptamine 6 (5‐HT₆) receptor antagonists based on 1‐thia‐4, 7‐diaza‐spiro[4.4]nonane‐3, 6‐dione motif has been disclosed. Enantiomers of potent racemate compound <bold>8a</bold> (K_i = 26 n<sc>m</sc>) displayed difference in activity (K_i of 15 n<sc>m</sc> versus 855 n<sc>m</sc>) signaling the influence of the stereochemistry of the chiral center on potency. In addition, the potent enantiomer displayed significant selectivity in biological activities over several related family members.</p> </abstract>