title: The synthesis and biological evaluation of non-peptidic matrix metalloproteinase inhibitors.
abstract: Novel sulfonamide matrix metalloproteinase inhibitors of general formula (9) were synthesised by a route involving a stereoselective conjugate addition reaction. Enzyme selectivity was found to be dependant on the nature of the sulfonamide substituents. Compounds (9f, 9q) are potent selective collagenase inhibitors with good oral bioavailability.
authors.affiliation: British Biotech Pharmaceuticals Limited, Cowley, Oxford. martinf@britbio.co.uk
authors.forename: F M
authors.initials: FM
authors.lastname: Martin
authors.forename: R P
authors.initials: RP
authors.lastname: Beckett
authors.forename: C L
authors.initials: CL
authors.lastname: Bellamy
authors.forename: P F
authors.initials: PF
authors.lastname: Courtney
authors.forename: S J
authors.initials: SJ
authors.lastname: Davies
authors.forename: A H
authors.initials: AH
authors.lastname: Drummond
authors.forename: R
authors.initials: R
authors.lastname: Dodd
authors.forename: L M
authors.initials: LM
authors.lastname: Pratt
authors.forename: S R
authors.initials: SR
authors.lastname: Patel
authors.forename: M L
authors.initials: ML
authors.lastname: Ricketts
authors.forename: R S
authors.initials: RS
authors.lastname: Todd
authors.forename: A R
authors.initials: AR
authors.lastname: Tuffnell
authors.forename: J W
authors.initials: JW
authors.lastname: Ward
authors.forename: M
authors.initials: M
authors.lastname: Whittaker
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001682:Biological Availability; D006860:Hydrogen Bonding; D006877:Hydroxamic Acids / Q000737:chemistry / Q000494:pharmacology; D061965:Matrix Metalloproteinase Inhibitors; D015394:Molecular Structure; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D006877:Hydroxamic Acids; D061965:Matrix Metalloproteinase Inhibitors; D011480:Protease Inhibitors; D013449:Sulfonamides; C100342:marimastat