SYNTHESIS OF PROLYL ENDOPEPTIDASE INHIBITORS AND EVALUATION OF THEIR STRUCTURE-ACTIVITY-RELATIONSHIPS - IN-VITRO INHIBITION OF PROLYL ENDOPEPTIDASE FROM CANINE BRAIN

被引：0
|
作者：
ARAI, H
NISHIOKA, H
NIWA, S
YAMANAKA, T
TANAKA, Y
YOSHINAGA, K
KOBAYASHI, N
MIURA, N
IKEDA, Y
机构：
来源：
CHEMICAL & PHARMACEUTICAL BULLETIN | 1993年 / 41卷 / 09期
关键词：
PROLYL ENDOPEPTIDASE; INHIBITOR; STRUCTURE ACTIVITY RELATIONSHIP; 4-PHENYLBUTANOYL DERIVATIVE; 4-(2-THIENYL)BUTANOYL DERIVATIVE;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
By chemical modification (of a known prolyl endopeptidase (PEP) inhibitor (N-[N-(4-phenylbutanoyl)-L-prolyl]pyrrolidine; SUAM-1221), several arylalkanoyl derivatives (V-1-27) were synthesized and tested for in vitro inhibitory activity towards PEP from canine brain. Among them, 4-(2-thienyl)butanoyl derivatives (V-24-27) showed more potent PEP-inhibitory activity than SUAM-1221. The structure-activity relationships of these compounds are discussed.
引用
收藏
页码：1583 / 1588
页数：6
相关论文
共 50 条
  • [31] Synthesis of Kynapcins and Telephoric Acids as Prolyl Endopeptidase Inhibitors of Anti-Dementia Drugs
    Lee, Yean-Jang
    Lin, S. -Y.
    BIOPHYSICAL JOURNAL, 2010, 98 (03) : 463A - 463A
  • [32] POST-PROLINE CLEAVING ENZYME (PROLYL ENDOPEPTIDASE) FROM BOVINE BRAIN
    YOSHIMOTO, T
    NISHIMURA, T
    KITA, T
    TSURU, D
    JOURNAL OF BIOCHEMISTRY, 1983, 94 (04): : 1179 - 1190
  • [33] Isolation and characterization of prolyl endopeptidase-inhibiting peptides from bovine brain
    Maruyama, S
    Ohmori, T
    PEPTIDE SCIENCE - PRESENT AND FUTURE, 1999, : 637 - 638
  • [34] Chemical constituents from Parrotia persica- Structural derivatization and their potential prolyl endopeptidase inhibition activity
    Ali, Hassan
    Ullah, Khair
    Siddiqui, Hina
    Iqbal, Shazia
    Atia-tul-Wahab
    Goren, Nezhun
    Ayatollahi, Seyed Abdulmajid
    Atta-ur-Rahman
    Choudhary, M. Iqbal
    BIOORGANIC CHEMISTRY, 2020, 96
  • [35] Characterization and crystal structure of prolyl endopeptidase from abalone (Haliotis discus hannai)
    Li, Wan-Yu
    Li, Yue
    Chen, Yu-Lei
    Hu, Jian-Jian
    Mengist, Hylemariam Mihiretie
    Liu, Guang-Ming
    Jin, Tengchuan
    Cao, Min-Jie
    FOOD CHEMISTRY, 2020, 333
  • [36] Inhibition of Eurygaster Integriceps Puton Prolyl Endoprotease (spPEP) and Human Prolyl Endopeptidase (hPEP) using αS1-Casein Peptide Inhibitors
    Kadakova, Petra
    FASEB JOURNAL, 2017, 31
  • [37] EVALUATION OF THE ROLE OF PROLYL ENDOPEPTIDASE AND PYROGLUTAMYL PEPTIDASE-I IN THE METABOLISM OF LHRH AND TRH IN BRAIN
    MENDEZ, M
    CRUZ, C
    JOSEPHBRAVO, P
    WILK, S
    CHARLI, JL
    NEUROPEPTIDES, 1990, 17 (02) : 55 - 62
  • [38] Ontogeny of soluble and particulate prolyl endopeptidase activity in several areas of the rat brain and in the pituitary gland
    Agirregoitia, N
    Irazusta, A
    Ruiz, F
    Irazusta, J
    Gil, J
    DEVELOPMENTAL NEUROSCIENCE, 2003, 25 (05) : 316 - 323
  • [39] Prolyl endopeptidase inhibitors from the underground part of Rhodiola sacra S.H.!Fu
    Fan, WZ
    Tezuka, Y
    Komatsu, K
    Namba, T
    Kadota, S
    BIOLOGICAL & PHARMACEUTICAL BULLETIN, 1999, 22 (02) : 157 - 161
  • [40] Purification of a prolyl endopeptidase from Aspergillus oryzae and evaluation of its ability to digest gluten
    Riggle, Heather M.
    Fisher, Matthew A.
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2009, 237
12345