From an Atypical Wake‐promoting Agent to Potent Histamine‐3 Receptor Inverse Agonists. (13th February 2013)

• Record Type: Journal Article
• Authors: Dunn, Derek; Raddatz, Rita; Ator, Mark A.; Bacon, Edward R.; Chatterjee, Sankar
• Is Part Of: Chemical biology & drug design. Volume 81:Number 3(2013:Mar.)
• Page Start: 433
• Page End: 435
• Publication Date: 2013-02-13
• Subjects: Drugs -- Design -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; 615.19005
• DOI: 10.1111/cbdd.12094
• Languages: English
• ISSNs: 1747-0277

Abstract

<abstract abstract-type="main" xml:lang="en"> <title> <x xml:space="preserve">Abstract</x> </title> <p>Utilizing atypical wake‐promoting agent modafinil (inactive in both rH₃ and hH₃ binding assays) as a launching pad, a series of sulfinyl‐ and sulfone‐derived H₃ receptor inverse agonists were developed. Brain‐permeable compound <bold>27</bold>, a potent member of the series displayed excellent selectivity against related family members (H₁, H_2, and H₄ receptors).</p> </abstract>