title: Benzodiazepine inhibitors of the MMPs and TACE. Part 2.
abstract: A series of benzodiazepine MMP/TACE inhibitors bearing polar moieties has been synthesized in an effort to optimize inhibitory activity against LPS-stimulated TNF production in human monocytes and oral activity in a murine LPS model.
authors.affiliation: Wyeth Research, 401N. Middletown Road, Pearl River, NY 10965, USA. levinji@wyeth.com
authors.forename: Jeremy I
authors.initials: JI
authors.lastname: Levin
authors.forename: Frances C
authors.initials: FC
authors.lastname: Nelson
authors.forename: Efren
authors.initials: E
authors.lastname: Delos Santos
authors.forename: Mila T
authors.initials: MT
authors.lastname: Du
authors.forename: Gloria
authors.initials: G
authors.lastname: MacEwan
authors.forename: James M
authors.initials: JM
authors.lastname: Chen
authors.forename: Semiramis
authors.initials: S
authors.lastname: Ayral-Kaloustian
authors.forename: Jun
authors.initials: J
authors.lastname: Xu
authors.forename: Guixian
authors.initials: G
authors.lastname: Jin
authors.forename: Terri
authors.initials: T
authors.lastname: Cummons
authors.forename: Dauphine
authors.initials: D
authors.lastname: Barone
mesh_terms: D051722:ADAM Proteins; D000072198:ADAM17 Protein; D000818:Animals; D001569:Benzodiazepines / Q000494:pharmacology*; D002460:Cell Line; D004791:Enzyme Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology*; D006801:Humans; D008070:Lipopolysaccharides / Q000494:pharmacology; D061965:Matrix Metalloproteinase Inhibitors; D008666:Metalloendopeptidases / Q000037:antagonists & inhibitors*; D051379:Mice; D008807:Mice, Inbred BALB C; D009000:Monocytes / Q000187:drug effects / Q000378:metabolism; D009055:Mouth / Q000187:drug effects; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000096:biosynthesis
chemical_list: D004791:Enzyme Inhibitors; D008070:Lipopolysaccharides; D061965:Matrix Metalloproteinase Inhibitors; D014409:Tumor Necrosis Factor-alpha; D001569:Benzodiazepines; D051722:ADAM Proteins; D008666:Metalloendopeptidases; D000072198:ADAM17 Protein; C000606462:ADAM17 protein, human; C000606463:Adam17 protein, mouse