2,3-Benzodiazepin-1,4-diones as peptidomimetic inhibitors of gamma-secretase.
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.
Prasad
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Department of Discovery Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, 5 Research Parkway, Wallingford, CT 06492, USA. prasad.chaturvedula@bms.com
Vig
Shikha
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Smith
David W
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Gao
Qi
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Polson
Craig T
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Corsa
Jason A
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Guss
Valerie L
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Loo
Alice
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Barten
Donna M
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Zheng
Ming
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Felsenstein
Kevin M
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Roberts
Susan B
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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
D000577:Amides; D007659:Ketones; D011480:Protease Inhibitors; D001569:Benzodiazepines; D053829:Amyloid Precursor Protein Secretases; D010450:Endopeptidases; D016282:Aspartic Acid Endopeptidases; C509282:Bace1 protein, mouse