title: Thiazole-diamides as potent gamma-secretase inhibitors.
abstract: The thiazole-diamide series (1) has been identified as highly potent gamma-secretase inhibitors. Several representative compounds showed IC(50) values of <0.3 nM. The synthesis and SAR, as well as a radiolabeled synthesis of [(3)H]-2a, are described.
authors.affiliation: Department of Medicinal Chemistry, PGRD, Pfizer Inc., Connecticut, Groton, CT 06340, USA. yuhpyng888@yahoo.com
authors.forename: Yuhpyng L
authors.initials: YL
authors.lastname: Chen
authors.forename: Kevin
authors.initials: K
authors.lastname: Cherry
authors.forename: Michael L
authors.initials: ML
authors.lastname: Corman
authors.forename: Charles F
authors.initials: CF
authors.lastname: Ebbinghaus
authors.forename: Chandra B
authors.initials: CB
authors.lastname: Gamlath
authors.forename: Dane
authors.initials: D
authors.lastname: Liston
authors.forename: Barbara-Anne
authors.initials: BA
authors.lastname: Martin
authors.forename: Christine E
authors.initials: CE
authors.lastname: Oborski
authors.forename: Barbara G
authors.initials: BG
authors.lastname: Sahagan
mesh_terms: D000478:Alkylation; D000586:Amination; D053829:Amyloid Precursor Protein Secretases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D002474:Cell-Free System; D003958:Diamide / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry*
chemical_list: D013844:Thiazoles; D003958:Diamide; D053829:Amyloid Precursor Protein Secretases