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Succinyl Hydroxamates as Potent and Selective Non-Peptidic Inhibitors of Procollagen C-proteinase: Design, Synthesis, and Evaluation as Topically Applied, Dermal Anti-Scarring Agents

Simon Bailey, Paul V Fish, Stephane Billotte, Jon Bordner, Doris Greiling, Kim James, Andrew McElroy, James E Mills, Charlotte Reed, Robert Webster

Bioorg Med Chem Lett. 2008 Dec 15;18(24):6562-7.

PMID: 18945617

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP348622888 UK-383,367 UK-383,367 348622-88-8 Price
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