Source:http://linkedlifedata.com/resource/pubmed/id/18945617
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
24
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pubmed:dateCreated |
2008-11-25
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pubmed:abstractText |
Succinyl hydroxamates 1 and 2 are disclosed as novel series of potent and selective inhibitors of procollagen C-proteinase (PCP) which may have potential as anti-fibrotic agents. Carboxamide 7 demonstrated good PCP inhibition and had excellent selectivity over MMPs involved in wound healing. In addition, 7 was effective in a cell-based model of collagen deposition (fibroplasia model) and was very effective at penetrating human skin in vitro. Compound 7 (UK-383,367) was selected as a candidate for evaluation in clinical studies as a topically applied, dermal anti-scarring agent.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
1464-3405
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6562-7
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pubmed:meshHeading |
pubmed-meshheading:18945617-Administration, Cutaneous,
pubmed-meshheading:18945617-Bone Morphogenetic Protein 1,
pubmed-meshheading:18945617-Cell Line, Tumor,
pubmed-meshheading:18945617-Chemistry, Pharmaceutical,
pubmed-meshheading:18945617-Cicatrix,
pubmed-meshheading:18945617-Cicatrix, Hypertrophic,
pubmed-meshheading:18945617-Drug Design,
pubmed-meshheading:18945617-Epidermis,
pubmed-meshheading:18945617-Fibrosis,
pubmed-meshheading:18945617-Humans,
pubmed-meshheading:18945617-Hydroxamic Acids,
pubmed-meshheading:18945617-Inhibitory Concentration 50,
pubmed-meshheading:18945617-Models, Chemical,
pubmed-meshheading:18945617-Molecular Conformation,
pubmed-meshheading:18945617-Oxazoles
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pubmed:year |
2008
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pubmed:articleTitle |
Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents.
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pubmed:affiliation |
Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK. simon.bailey@pfizer.com
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pubmed:publicationType |
Journal Article
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