Design and synthesis of procollagen C-proteinase inhibitors
摘要:
Non-peptidic inhibitors of procollagen C-proteinase (PCP) were designed from substrate leads. Compounds were optimized for potency and selectivity, with N-substituted aryl sulfonamide hydroxamates having the best combination of these properties. Compounds 89 and 60 have IC50 values of 10 and 80 nM, respectively, against PCP; excellent selectivity over MMP's 1, 2, and 9; and activity in cell-based collagen deposition assays. (C) 2012 Elsevier Ltd. All rights reserved.
N-substituted arylsulfonylamino hydroxamic acids useful as inhibitors of c-proteinase and for treating or preventing disorders related to unregulated collagen production
N-substituted arylsulfonylamino hydroxamic acids useful as inhibitors of c-proteinase and for treating or preventing disorders related to unregulated collagen production
申请人:FibroGen, Inc.
公开号:US06506936B1
公开(公告)日:2003-01-14
The present invention relates to a novel class of organic molecules capable of inhibiting C-proteinase, and to their use to regulate, modulate and/or inhibit abnormal collagen formation as a therapeutic approach towards the treatment of fibrotic disorders.
N-substituted arylsulfonylamino hydroxamic acids useful as inhibitors of C-proteinase and for treating or preventing disorders related to unregulated collagen production
申请人:——
公开号:US20030191309A1
公开(公告)日:2003-10-09
The present invention relates to a novel class of organic molecules capable of inhibiting C-proteinase, and to their use to regulate, modulate and/or inhibit abnormal collagen formation as a therapeutic approach towards the treatment of fibrotic disorders.
Peptidomimetics of Efflux Pump Inhibitors Potentiate the Activity of Levofloxacin in Pseudomonas aeruginosa
作者:Thomas E. Renau、Roger Léger、Rose Yen、Miles W. She、Eric M. Flamme、Joan Sangalang、Carla L. Gannon、Suzanne Chamberland、Olga Lomovskaya、Ving J. Lee
DOI:10.1016/s0960-894x(02)00006-9
日期:2002.3
Several classes of peptidomimetics of the efflux pump inhibitor D-ornithine-D-homophenylalanine-3-aminoquinoline (MC-02,595) have been prepared and evaluated for their ability to potentiate the activity of the fluoroquinolone levofloxacin in Pseudomonas aeruginosa. A number of the new analogues were as active or more active than the lead. demonstrating that a peptide backbone is not essential for activity. (C) 2002 Elsevier Science Ltd. All rights reserved.
Pyrimidines LIX. Synthesis and biological properties of N-substituted dihydrouracils and dihydrothiouracils
作者:M. A. Kaldrikyan、V. A. Geboyan、G. M. Stepanyan、B. T. Garibdzhanyan、R. V. Paronikyan、Yu. Z. Ter-Zakharyan、L. G. Akopyan、G. M. Paronikyan
DOI:10.1007/bf00765024
日期:1983.10
N-ACYLPIPERIDINYLCARBONYLAMINOCARBOXYLIC ACIDS AND THEIR USE AS GLYCOPROTEIN IIB/IIa ANTAGONISTS AND FIBRINOGEN-BLOOD PLATELETS BINDING INHIBITORS