Novel Inhibitors of Procollagen C-Terminal Proteinase. Part 1: Diamino Acid Hydroxamates

The parallel synthesis of novel inhibitors of procollagen C-terminal proteinase is described. The synthetic strategy allowed for the facile synthesis of a large number of side-chain diversified diamino acid hydroxamates, of which the d-diaminopropionic acid derivatives were shown to be single digit...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-07, Vol.13 (13), p.2101-2104
Main Authors: Delaet, N.G.J., Robinson, L.A., Wilson, D.M., Sullivan, R.W., Bradley, E.K., Dankwardt, S.M., Martin, R.L., Van Wart, H.E., Walker, K.A.M.
Format: Article
Language:English
Subjects:
Analytical, structural and metabolic biochemistry
Biological and medical sciences
Bone Morphogenetic Protein 1
Bone Morphogenetic Proteins - antagonists & inhibitors
Enzymes and enzyme inhibitors
Fundamental and applied biological sciences. Psychology
Hydrolases
Hydroxamic Acids - chemical synthesis
Hydroxamic Acids - pharmacology
Indicators and Reagents
Kinetics
Medical sciences
Metalloendopeptidases - antagonists & inhibitors
Miscellaneous
Pharmacology. Drug treatments
Protease Inhibitors - chemical synthesis
Protease Inhibitors - pharmacology
Structure-Activity Relationship
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Summary:The parallel synthesis of novel inhibitors of procollagen C-terminal proteinase is described. The synthetic strategy allowed for the facile synthesis of a large number of side-chain diversified diamino acid hydroxamates, of which the d-diaminopropionic acid derivatives were shown to be single digit nanomolar PCP inhibitors. The parallel synthesis and SAR studies of diamino acid hydroxamate inhibitors of procollagen C-terminal proteinase are reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(03)00404-9