Synthesis and biological activity of novel potent endothelin-converting enzyme-1 inhibitors

被引：12
|
作者：
Firooznia, F [1 ]
Gude, C [1 ]
Chan, K [1 ]
Fink, CA [1 ]
Qiao, Y [1 ]
Satoh, Y [1 ]
Marcopoulos, N [1 ]
Savage, P [1 ]
Beil, ME [1 ]
Bruseo, CW [1 ]
Trapani, AJ [1 ]
Jeng, AY [1 ]
机构：
[1] Novartis Inst Biomed Res, Summit, NJ 07901 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 03期
关键词：
D O I：
10.1016/S0960-894X(00)00657-0
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Through directed screening of metalloprotease inhibitors. CGS 30084 (1) has been identified as a potent endothelin-converting enzyme-1 (ECE-1) inhibitor in vitro (IC50 = 77 nM). Herein we report the synthesis and biological activities of analogues derived from this lead. based on modifications of the biphenyl moiety. Compound 10. the thioacetate methyl ester prodrug derivative of compound 6m. was found to he an orally active and potent inhibitor of ECE-1 activity in rats. (C) 2001 Elsevier science Ltd. All rights reserved.
引用
收藏
页码：375 / 378
页数：4
相关论文
共 50 条
  • [21] Cellular distribution of endothelin-converting enzyme-1 in human tissues
    Korth, P
    Bohle, RM
    Corvol, P
    Pinet, F
    JOURNAL OF HISTOCHEMISTRY & CYTOCHEMISTRY, 1999, 47 (04) : 447 - 461
  • [22] Phosphinic Tripeptides as Dual Angiotensin-Converting Enzyme C-Domain and Endothelin-Converting Enzyme-1 Inhibitors
    Jullien, Nicolas
    Makritis, Anastasios
    Georgiadis, Dimitris
    Beau, Fabrice
    Yiotakis, Athanasios
    Dive, Vincent
    JOURNAL OF MEDICINAL CHEMISTRY, 2010, 53 (01) : 208 - 220
  • [23] Synthesis of novel substituted pyridines as inhibitors of endothelin converting enzyme-1 (ECE-1)
    Massa, MA
    Patt, WC
    Ahn, K
    Sisneros, AM
    Herman, SB
    Doherty, A
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (16) : 2117 - 2122
  • [24] Protein kinase C regulates the cell surface activity of endothelin-converting enzyme-1
    Smith, A. Ian
    Lew, Rebecca A.
    Thomas, Walter G.
    Tochon-Danguy, Nathalie
    INTERNATIONAL JOURNAL OF PEPTIDE RESEARCH AND THERAPEUTICS, 2006, 12 (03) : 291 - 295
  • [25] Protein Kinase C Regulates the Cell Surface Activity of Endothelin-Converting Enzyme-1
    A. Ian Smith
    Rebecca A. Lew
    Walter G. Thomas
    Nathalie Tochon-Danguy
    International Journal of Peptide Research and Therapeutics, 2006, 12 : 291 - 295
  • [26] Distribution of endothelin-converting enzyme-1 and neutral endopeptidase in human endometrium
    Iwase, Akira
    Ando, Hisao
    Nagasaka, Tetsuro
    Goto, Maki
    Harata, Toko
    Kikkawa, Fumitaka
    JOURNAL OF HISTOCHEMISTRY & CYTOCHEMISTRY, 2007, 55 (12) : 1229 - 1235
  • [27] Hyperinsulinemia Increases Placenta Endothelin-Converting Enzyme-1 Expression in Trophoblasts
    Khamaisi, Mogher
    Skarzinski, Galia
    Mekler, Judith
    Zreik, Farid
    Damouni, Rawan
    Ariel, Ilana
    Bursztyn, Michael
    AMERICAN JOURNAL OF HYPERTENSION, 2012, 25 (01) : 109 - 114
  • [28] Endothelin-converting enzyme-1 mRNA expression in human cardiovascular disease
    Bohnemeier, H
    Pinto, YM
    Horkay, F
    Tóth, M
    Juhász-Nagy, A
    Orzechowski, HD
    Paul, M
    JOURNAL OF CARDIOVASCULAR PHARMACOLOGY, 1998, 31 : S52 - S54
  • [29] Regulation of endothelin-converting enzyme-1 expression in human neuroblastoma cells
    Fisk, Lilia
    Nalivaeva, Natalia N.
    Turner, Anthony J.
    EXPERIMENTAL BIOLOGY AND MEDICINE, 2006, 231 (06) : 1048 - 1053
  • [30] Endothelin-converting enzyme-1 in Alzheimer's disease and vascular dementia
    Palmer, J. C.
    Kehoe, P. G.
    Love, S.
    NEUROPATHOLOGY AND APPLIED NEUROBIOLOGY, 2010, 36 (06) : 487 - 497
12345