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
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.
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