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
  • [1] NEW POTENT PROLYL ENDOPEPTIDASE INHIBITORS - SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF INDAN AND TETRALIN DERIVATIVES AND THEIR ANALOGS
    TANAKA, Y
    NIWA, S
    NISHIOKA, H
    YAMANAKA, T
    TORIZUKA, M
    YOSHINAGA, K
    KOBAYASHI, N
    IKEDA, Y
    ARAI, H
    JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (13) : 2071 - 2078
  • [2] SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF PEPTIDYL ALPHA-KETO HETEROCYCLES AS NOVEL INHIBITORS OF PROLYL ENDOPEPTIDASE
    TSUTSUMI, S
    OKONOGI, T
    SHIBAHARA, S
    OHUCHI, S
    HATSUSHIBA, E
    PATCHETT, AA
    CHRISTENSEN, BG
    JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (21) : 3492 - 3502
  • [3] STRUCTURE ACTIVITY RELATIONSHIP OF INHIBITORS SPECIFIC FOR PROLYL ENDOPEPTIDASE
    YOSHIMOTO, T
    TSURU, D
    YAMAMOTO, N
    IKEZAWA, R
    FURUKAWA, S
    AGRICULTURAL AND BIOLOGICAL CHEMISTRY, 1991, 55 (01): : 37 - 43
  • [4] ON PSYCHOTROPIC PROPERTIES OF BRAIN PROLYL ENDOPEPTIDASE INHIBITORS
    ZOLOTOV, NN
    NARKEVICH, VB
    POZDNEV, VF
    PRIKHOZHAN, AV
    VORONINA, TA
    RAYEVSKII, KS
    DOKLADY AKADEMII NAUK SSSR, 1992, 322 (04): : 776 - 779
  • [5] SYNTHESIS OF PEPTIDYL ACETALS AS INHIBITORS OF PROLYL ENDOPEPTIDASE
    AUGUSTYNS, K
    BORLOO, M
    BELYAEV, A
    RAJAN, P
    GOOSSENS, F
    HENDRIKS, D
    SCHARPE, S
    HAEMERS, A
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1995, 5 (12) : 1265 - 1270
  • [6] Synthesis and evaluation of succinic acid derivatives as prolyl endopeptidase inhibitors
    Seung-Bin Yoon
    Jae-Sung Yang
    Kyung-Ho Lee
    Hyeon-Gyu Han
    Ah-Reum Han
    Young-Sook Paik
    Journal of the Korean Society for Applied Biological Chemistry, 2011, 54 (5): : 731 - 737
  • [7] Synthesis and Evaluation of Succinic Acid Derivatives as Prolyl Endopeptidase Inhibitors
    Yoon, Seung-Bin
    Yang, Jae-Sung
    Lee, Kyung-Ho
    Han, Hyeon-Gyu
    Han, Ah-Reum
    Paik, Young-Sook
    JOURNAL OF THE KOREAN SOCIETY FOR APPLIED BIOLOGICAL CHEMISTRY, 2011, 54 (05): : 731 - 737
  • [8] Prolyl endopeptidase inhibitors derived from actinomycetes
    Kimura, K
    Kanou, F
    Yamashita, Y
    Yoshimoto, T
    Yoshihama, M
    BIOSCIENCE BIOTECHNOLOGY AND BIOCHEMISTRY, 1997, 61 (10) : 1754 - 1756
  • [9] Prolyl endopeptidase inhibitors from caryophylli flos
    Kyung-Hee Lee
    Jong Hwan Kwak
    Kyung-Bok Lee
    Kyung-Sik Song
    Archives of Pharmacal Research, 1998, 21 : 207 - 211
  • [10] Prolyl Endopeptidase inhibitors from green tea
    Jin-Hui Kim
    Sang-In Kim
    Kyung-Sik Song
    Archives of Pharmacal Research, 2001, 24 : 292 - 296
12345