cheminform abstract: succinyl hydroxamates as potent and selective non-peptidic inhibitors of...

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ChemInform 2009, 40, issue 17 © 2009 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim www.cheminform.wiley-vch.de Enzyme inhibiting activity X 0220 Succinyl Hydroxamates as Potent and Selective Non-peptidic Inhibitors of Procol- lagen C-Proteinase: Design, Synthesis and Evaluation as Topically Applied, Der- mal anti-Scarring Agents. — A novel series of compounds such as (I) is synthesized and the structure—activity relationship is discussed. Derivative (Ia), named UK-383,367 is selected as candidate for evaluation in clinical studies as a topically ap- plied, dermal anti-scarring agent. — (BAILEY*, S.; FISH, P. V.; BILLOTTE, S.; BORDNER, J.; GREILING, D.; JAMES, K.; MCELROY, A.; MILLS, J. E.; REED, C.; WEBSTER, R.; Bioorg. Med. Chem. Lett. 18 (2008) 24, 6562-6567; Dep. Chem., Pfizer Global Res. Dev., San Diego, CA 92121, USA; Eng.) — K. Schneider 17- 220

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Page 1: ChemInform Abstract: Succinyl Hydroxamates as Potent and Selective Non-peptidic Inhibitors of Procollagen C-Proteinase: Design, Synthesis and Evaluation as Topically Applied, Dermal

www.cheminform.wiley-vch.de

Enzyme inhibiting activityX 0220 Succinyl Hydroxamates as Potent and Selective Non-peptidic Inhibitors of Procol-

lagen C-Proteinase: Design, Synthesis and Evaluation as Topically Applied, Der-mal anti-Scarring Agents. — A novel series of compounds such as (I) is synthesized and the structure—activity relationship is discussed. Derivative (Ia), named UK-383,367 is selected as candidate for evaluation in clinical studies as a topically ap-plied, dermal anti-scarring agent. — (BAILEY*, S.; FISH, P. V.; BILLOTTE, S.; BORDNER, J.; GREILING, D.; JAMES, K.; MCELROY, A.; MILLS, J. E.; REED, C.; WEBSTER, R.; Bioorg. Med. Chem. Lett. 18 (2008) 24, 6562-6567; Dep. Chem., Pfizer Global Res. Dev., San Diego, CA 92121, USA; Eng.) — K. Schneider

17- 220

ChemInform 2009, 40, issue 17 © 2009 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim