In Search of Potent 5‐HT6 Receptor Inverse Agonists. (June 2014)

• Record Type: Journal Article
• Authors: Hostetler, Greg; Dunn, Derek; McKenna, Beth Ann; Kopec, Karla; Chatterjee, Sankar
• Is Part Of: Chemical biology & drug design. Volume 83:Number 6(2014:Jun.)
• Page Start: 666
• Page End: 669
• Publication Date: 2014-06
• Subjects: Drugs -- Design -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; 615.19005
• DOI: 10.1111/cbdd.12279
• Languages: English
• ISSNs: 1747-0277

Abstract

<abstract abstract-type="main" id="cbdd12279-abs-0001"> <title> <x xml:space="preserve">Abstract</x> </title> <p>A series of non‐sulfonamide/non‐sulfone derived potent 5‐HT₆ receptor inverse agonists has been disclosed. Representative compound <bold>9</bold> (<bold><italic>K</italic></bold>_i = 14 n<sc>m</sc>) displayed selectivity against a set of family members as well as brain permeability 6 h post‐oral administration. In addition, the separated enantiomers of compound <bold>9</bold> displayed difference in activity indicating the influence of chirality on potency.</p> </abstract>