Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents.

Bailey S; Fish PV; Billotte S; Bordner J; Greiling D; James K; McElroy A; Mills JE; Reed C; Webster R

首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >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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Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents.

机译：琥珀酸异羟肟酸酯作为前胶原C蛋白酶的有效和选择性非肽类抑制剂：设计，合成和评估为局部应用的皮肤抗瘢痕形成剂。

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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.

机译：公开了琥珀酸异羟肟酸酯1和2作为新系列的有效的和选择性的胶原蛋白C蛋白酶（PCP）抑制剂，其可能具有作为抗纤维化剂的潜力。羧酰胺7表现出良好的PCP抑制作用，对伤口愈合中涉及的MMP具有优异的选择性。另外，7在胶原蛋白沉积的基于细胞的模型（纤维化模型）中有效，并且在体外穿透人皮肤方面非常有效。选择化合物7（UK-383,367）作为局部应用的皮肤抗瘢痕形成剂，作为临床研究中的评估候选物。

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《Bioorganic and Medicinal Chemistry Letters》 |2008年第24期|共6页
作者
Bailey S; Fish PV; Billotte S; Bordner J; Greiling D; James K; McElroy A; Mills JE; Reed C; Webster R;
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正文语种 eng
中图分类药学;生物化学;
关键词
procollagen C-endopeptidase; inhibitors; Evaluation; hydroxamate;

机译：前胶原C-内肽酶;抑制剂;评估;异羟肟酸酯;

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1. Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents. [J] . Bailey S, Fish PV, Billotte S, Bioorganic and Medicinal Chemistry Letters . 2008,第24期

机译：琥珀酸异羟肟酸酯作为前胶原C蛋白酶的有效和选择性非肽类抑制剂：设计，合成和评估为局部应用的皮肤抗瘢痕形成剂。
2. Potent and Selective Nonpeptidic Inhibitors of Procollagen C-Proteinase [J] . Paul V. Fish, Gillian A. Allan, Simon Bailey Journal of Medicinal Chemistry . 2007,第15期

机译：胶原蛋白C蛋白酶的有效和选择性非肽类抑制剂
3. Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1). [J] . Fray MJ, Dickinson RP Bioorganic and Medicinal Chemistry Letters . 2001,第4期

机译：发现基质金属蛋白酶-3（间质溶素-1）的有效和选择性琥珀酰异羟肟酸酯抑制剂。
4. Design and Synthesis of Mercaptoacyl Dipeptides as Potent and Selective PHEX Inhibitors [C] . Elaref S. Ratemi, Denis Gravel, Philippe Crine American Peptide Symposium . 2009

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5. Design, synthesis, and biological evaluation of novel neo-tanshinlactone analogues as potent and selective anti-breast cancer agents. [D] . Dong, Yizhou. 2009

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6. Design Synthesis and Evaluation of Potent Non-Peptidic Mimetics of Second Mitochondria-derived Activator of Caspases [O] . Wei Sun, Zaneta Nikolovska-Coleska, Dongguang Qin, -1

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7. QSAR study of the non-peptidic inhibitors of procollagen C-proteinase based on Multiple linear regression, principle component regression, and partial least squares [O] . Ardeshir Khazaei, Negin Sarmasti, Jaber Yousefi Seyf, 2017

机译：基于多元线性回归，主成分回归和偏最小二乘法的QaaR研究前胶原C蛋白酶的非肽类抑制剂
8. Design, Synthesis and Study of Cell Adhesion Antagonists: Hydroxamate- Based Peptide Inhibitors of avb3 Integrin [R] . Hwu, C. , Harvey, D. 2000

机译：细胞粘附拮抗剂的设计，合成和研究：基于异羟肟酸的avb3整合素肽抑制剂

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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