N-(INDOL-3-YLGLYOXYLYL)AMINO ACID ESTER DERIVATIVES - SYNTHESIS AND INTERACTION PROPERTIES AT THE BENZODIAZEPINE RECEPTOR

被引:0
|
作者
PRIMOFIORE, G [1 ]
DASETTIMO, F [1 ]
MARINI, AM [1 ]
LAMOTTA, C [1 ]
MARTINI, C [1 ]
SENATORE, G [1 ]
LUCACCHINI, A [1 ]
机构
[1] UNIV PISA, IST POLICATTEDRA DISCIPLINE BIOL, I-56126 PISA, ITALY
来源
FARMACO | 1995年 / 50卷 / 01期
关键词
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Several N-(indol-3-ylglyoxylyl)alanine and glycine ester derivatives were prepared to evaluate the influence of the ester group size both on affinity and on activity at the benzodiazepine receptor. Moreover, indol-3-ylglyoxylic acid esters, closely related to 3-alkoxy-beta-carbolines, were synthesized and tested in vitro on the benzodiazepine receptor.
引用
收藏
页码:5 / 12
页数:8
相关论文
共 50 条
  • [21] Synthesis of N-[(β-carboline-3-yl)-formyl]-L-amino acid derivatives
    Wang, C
    Peng, SQ
    Yang, M
    [J]. HETEROCYCLIC COMMUNICATIONS, 1998, 4 (02) : 181 - 186
  • [22] N-(INDOLE-3-YLGLYOXYL) AMINO-ACID DERIVATIVES - PREPARATION AND PHARMACOLOGICAL PROPERTIES
    DASETTIMO, A
    PRIMOFIORE, G
    MARINI, AM
    TONETTI, I
    FERRARINI, PL
    FRANZONE, JS
    CIRILLO, R
    BADINI, C
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1984, 19 (06) : 507 - 511
  • [23] Synthesis of N-(3-arylpropyl)amino acid derivatives by sonogashira types of reaction in aqueous media
    López-Deber, MP
    Castedo, L
    Granja, JR
    [J]. ORGANIC LETTERS, 2001, 3 (18) : 2823 - 2826
  • [24] L-amino acid esters studies: Part I: Synthesis of new methyl N-(dimethoxy/3,5-diacetoxybenzoyl)-L-amino acid ester derivatives.
    Al-Afaleq, EI
    Abubshait, SA
    [J]. SYNTHETIC COMMUNICATIONS, 1999, 29 (11) : 1965 - 1976
  • [25] Refinement of the benzodiazepine receptor site topology by structure-activity relationships of new N-(heteroarylmethyl)indol-3-ylglyoxylamides
    Primofiore, G
    Da Settimo, F
    Marini, AM
    Taliani, S
    La Motta, C
    Simorini, F
    Novellino, E
    Greco, G
    Cosimelli, B
    Ehlardo, M
    Sala, A
    Besnard, F
    Montali, M
    Martini, C
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2006, 49 (08) : 2489 - 2495
  • [26] Synthesis of N-(methoxycarbonyl or isopropylcarbamoyl-methoxyphosphonyl)-alpha-amino acid ester and their stereomers
    Chen, RY
    Li, HY
    [J]. SCIENCE IN CHINA SERIES B-CHEMISTRY, 1996, 39 (04): : 371 - 377
  • [27] Novel phosphonoacetic acid derivatives.: Synthesis of N-(ethoxycarbonylmethylphosphonyl)-α-amino acid esters and -α-amino phosphonic acid esters and their bioactivities
    Li, HY
    Ren, KT
    Chen, RY
    [J]. CHINESE CHEMICAL LETTERS, 1997, 8 (12) : 1047 - 1050
  • [28] Synthesis of N-substituted derivatives of (5-amino-2-methyl-1H-indol-3-YL)acetic acid
    Maklakov S.A.
    Smushkevich Yu.I.
    Magedov I.V.
    [J]. Chemistry of Heterocyclic Compounds, 2002, 38 (5) : 539 - 542
  • [29] Novel N-(arylalkyl) indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor:: Synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships
    Primofiore, G
    Da Settimo, F
    Taliani, S
    Marini, AM
    Novellino, E
    Greco, G
    Lavecchia, A
    Besnard, F
    Trincavelli, L
    Costa, B
    Martini, C
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2001, 44 (14) : 2286 - 2297
  • [30] Novel Phosphonoacetic Acid Derivatives.Synthesis of N-(Ethoxycarbonylmethylphosphonyl)-α-Amino Esters and-α-Amino Phosphonic Acid Esters and Their Bioactivities
    Hui Ying LI
    Kang Tai REN
    Ru Yu CHEN(Institute of Elemento-Organic Chemistry
    [J]. Chinese Chemical Letters, 1997, (12) : 0 - 0