Oxal hydroxamic acid derivatives with inhibitory activity against matrix metalloproteinases.
Several amines, amino acid derivatives and low molecular weight peptides containing an amide-bound oxal hydroxamic acid moiety have been synthesized and tested for their inhibitory effects towards native human gelatinase B (MMP-9) and the catalytic domains of the membrane type MT1-MMP (MMP-14) and of neutrophil collagenase (MMP-8). A number of these compounds exhibited considerable inhibitory activity against the tested metalloproteinases.
Krumme
Dirk
D
University of Bielefeld, Department Biochemie I, Universitätsstrasse 25, D-33615, Bielefeld, Germany. dkr@gbf.de
Tschesche
Harald
H
D000588:Amines / Q000138:chemical synthesis / Q000494:pharmacology; D000596:Amino Acids / Q000138:chemical synthesis / Q000494:pharmacology; D020134:Catalytic Domain; D006801:Humans; D006877:Hydroxamic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D020784:Matrix Metalloproteinase 8 / Q000737:chemistry; D020780:Matrix Metalloproteinase 9 / Q000737:chemistry; D061965:Matrix Metalloproteinase Inhibitors; D020782:Matrix Metalloproteinases / Q000737:chemistry; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000588:Amines; D000596:Amino Acids; D006877:Hydroxamic Acids; D061965:Matrix Metalloproteinase Inhibitors; D009842:Oligopeptides; D020782:Matrix Metalloproteinases; D020784:Matrix Metalloproteinase 8; D020780:Matrix Metalloproteinase 9