Details

Autor(en) / Beteiligte

• Burnett, Duane A
• Caplen, Mary Ann
• Domalski, Martin S
• Browne, Margaret E
• Davis, Jr, Harry R
• Clader, John W

Titel

Synthesis of iodinated biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2002-02, Vol.12 (3), p.311-314

Ort / Verlag

Oxford: Elsevier Ltd

Erscheinungsjahr

2002

Quelle

Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)

Beschreibungen/Notizen

• The discoveries of Sch 48461 and Sch 58235 and their novel pharmacology of inhibition of cholesterol absorption have prompted efforts to determine their biological mechanism of action (MOA). To this end, a series of radioiodinated analogues with good to excellent in vivo activity have been designed and synthesized as single enantiomers. They are structurally consistent with the allowable SAR of the 2-azetidinone class of cholesterol absorption inhibitors. The discoveries of Sch 48461 and Sch 58235 and their novel pharmacology of inhibition of cholesterol absorption have prompted efforts to determine their biological mechanism of action (MOA). To this end, a series of radioiodinated analogues with good to excellent in vivo activity have been designed and synthesized as single enantiomers. They are structurally consistent with the allowable SAR of the 2-azetidinone class of cholesterol absorption inhibitors.