Highly potent and selective inhibitors of endothelin converting enzyme

被引:25
作者
Chackalamannil, S
Chung, S
Stamford, AW
McKittrick, BA
Wang, YG
Tsai, HG
Cleven, R
Fawzi, A
Czarniecki, M
机构
[1] Schering-Plough Research Institute, Kenilworth, NJ 07033
关键词
D O I
10.1016/0960-894X(96)00211-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Phosphinic acid derivatives, represented by structure 1, have been synthesized and evaluated as endothelin converting enzyme (ECE) inhibitors. Several of these compounds (for example, 1b, 1c, and 1f) were found to be potent inhibitors of ECE with a high degree of selectivity against neutral endopeptidase (NEP). Copyright (C) 1996 Elsevier Science Ltd.
引用
收藏
页码:1257 / 1260
页数:4
相关论文
共 15 条
  • [1] ENDOTHELIN - A KNOCKOUT IN LONDON
    BATTISTINI, B
    BOTTING, R
    WARNER, TD
    [J]. TRENDS IN PHARMACOLOGICAL SCIENCES, 1995, 16 (07) : 217 - 222
  • [2] 1-AMINOALKYLPHOSPHONOUS ACIDS .1. ISOSTERES OF THE PROTEIN AMINO-ACIDS
    BAYLIS, EK
    CAMPBELL, CD
    DINGWALL, JG
    [J]. JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1, 1984, (12): : 2845 - 2853
  • [3] PHOSPHORUS-CONTAINING INHIBITORS OF ENDOTHELIN CONVERTING ENZYME - EFFECTS OF THE ELECTRONIC NATURE OF PHOSPHORUS ON INHIBITOR POTENCY
    BERTENSHAW, SR
    ROGERS, RS
    STERN, MK
    NORMAN, BH
    MOORE, WM
    JEROME, GM
    BRANSON, LM
    MCDONALD, JF
    MCMAHON, EG
    PALOMO, MA
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (01) : 173 - 176
  • [4] THIOL AND HYDROXAMIC ACID-CONTAINING INHIBITORS OF ENDOTHELIN-CONVERTING ENZYME
    BERTENSHAW, SR
    TALLEY, JJ
    ROGERS, RS
    CARTER, JS
    MOORE, WM
    BRANSON, LM
    KOBOLDT, CM
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (10) : 1953 - 1958
  • [5] HYDROXAMIC ACIDS AS POTENT INHIBITORS OF ENDOTHELIN-CONVERTING ENZYME FROM HUMAN BRONCHIOLAR SMOOTH-MUSCLE
    BIHOVSKY, R
    LEVINSON, BL
    LOEWI, RC
    ERHARDT, PW
    POLOKOFF, MA
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (12) : 2119 - 2129
  • [6] EFFECT OF AN ENDOTHELIN-RECEPTOR ANTAGONIST ON ISCHEMIC ACUTE-RENAL-FAILURE
    CHAN, L
    CHITTINANDANA, A
    SHAPIRO, JI
    SHANLEY, PF
    SCHRIER, RW
    [J]. AMERICAN JOURNAL OF PHYSIOLOGY, 1994, 266 (01): : F135 - F138
  • [7] ENDOTHELIN - A NEW CHALLENGE
    DOHERTY, AM
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (09) : 1493 - 1508
  • [8] EPSTEIN FH, 1995, NEW ENGL J MED, V333, P356
  • [9] A RAPID AND SELECTIVE ENDOTHELIN-CONVERTING ENZYME ASSAY - CHARACTERIZATION OF A PHOSPHORAMIDON-SENSITIVE ENZYME FROM GUINEA-PIG LUNG MEMBRANE
    FAWZI, AB
    CLEVEN, RM
    WRIGHT, DL
    [J]. ANALYTICAL BIOCHEMISTRY, 1994, 222 (02) : 342 - 350
  • [10] AMINOPHOSPHONATE ENDOTHELIN-CONVERTING ENZYME-INHIBITORS - POTENCY-ENHANCING AND SELECTIVITY-IMPROVING MODIFICATIONS OF PHOSPHORAMIDON
    FUKAMI, T
    HAYAMA, T
    AMANO, Y
    NAKAMURA, Y
    ARAI, Y
    MATSUYAMA, K
    YANO, M
    ISHIKAWA, K
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1994, 4 (10) : 1257 - 1262