Identification of nonabsorbable inhibitors of the scavenger receptor-BI (SR-BI) for tissue-specific administration. Issue 8 (15th April 2016)

• Record Type: Journal Article
• Authors: Sparks, Steven M.; Zhou, Huiqiang; Generaux, Claudia; Harston, Lindsey; Moncol, David; Jayawickreme, Channa; Parham, Janet; Condreay, Patrick; Rimele, Thomas
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 8(2016)
• Page Start: 1901
• Page End: 1904
• Publication Date: 2016-04-15
• Subjects: Scavenger receptor class B type I -- SR-BI inhibitor -- Nonabsorbed SR-BI inhibitor -- Intestinal SR-BI; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.03.025
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: The identification of a low-permeability scavenger receptor BI (SR-BI) inhibitor starting from the ITX-5061 template is described. Structure–activity and structure–permeability relationships were assessed for analogs leading to the identification of compound8 as a potent and nonabsorbable SR-BI inhibitor.