title: 2,3-Benzodiazepin-1,4-diones as peptidomimetic inhibitors of gamma-secretase.
abstract: 2,3-Benzodiazepin-1,4-diones were designed as peptidomimetics at the carboxy terminus of hydroxyamides. Inhibition of brain Abeta production was improved by one of the compounds containing constrained modification.
authors.affiliation: Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. prasad.chaturvedula@bms.com
authors.forename: C V C
authors.initials: CV
authors.lastname: Prasad
authors.forename: Shikha
authors.initials: S
authors.lastname: Vig
authors.forename: David W
authors.initials: DW
authors.lastname: Smith
authors.forename: Qi
authors.initials: Q
authors.lastname: Gao
authors.forename: Craig T
authors.initials: CT
authors.lastname: Polson
authors.forename: Jason A
authors.initials: JA
authors.lastname: Corsa
authors.forename: Valerie L
authors.initials: VL
authors.lastname: Guss
authors.forename: Alice
authors.initials: A
authors.lastname: Loo
authors.forename: Donna M
authors.initials: DM
authors.lastname: Barten
authors.forename: Ming
authors.initials: M
authors.lastname: Zheng
authors.forename: Kevin M
authors.initials: KM
authors.lastname: Felsenstein
authors.forename: Susan B
authors.initials: SB
authors.lastname: Roberts
mesh_terms: D000544:Alzheimer Disease / Q000201:enzymology; D000577:Amides / Q000737:chemistry; D053829:Amyloid Precursor Protein Secretases; D000818:Animals; D016282:Aspartic Acid Endopeptidases; D001569:Benzodiazepines / Q000138:chemical synthesis / Q000494:pharmacology; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D002460:Cell Line; D015195:Drug Design; D010450:Endopeptidases / Q000378:metabolism*; D020128:Inhibitory Concentration 50; D007659:Ketones / Q000138:chemical synthesis / Q000494:pharmacology; D051379:Mice; D008968:Molecular Conformation; D018716:Molecular Mimicry; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology*; D011485:Protein Binding
chemical_list: D000577:Amides; D007659:Ketones; D011480:Protease Inhibitors; D001569:Benzodiazepines; D053829:Amyloid Precursor Protein Secretases; D010450:Endopeptidases; D016282:Aspartic Acid Endopeptidases; C509282:Bace1 protein, mouse