CONFORMATIONALLY RESTRICTED PIPERIDINYL BENZAMIDES AS 5-HT3 RECEPTOR ANTAGONISTS

被引:5
|
作者
BERMUDEZ, J
HADLEY, MS
KING, FD
MARTIN, RT
机构
[1] SmithKline Beecham Pharmaceuticals, Harlow, Essex CM19 5AD, Coldharbour Road, The Pinnacles
关键词
D O I
10.1016/S0960-894X(01)81190-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and 5-HT3 receptor antagonist activity of indolizidin-7-yl and 8-oxaquinolizidin-2-yl benzamides related to the quinolizidine, BRL 20627 (2), are described. High potency is restricted to axial isomers and both the indolizidines and oxa-quinolizidines are much more potent than (2), an effect which appears to be unrelated to basicity.
引用
收藏
页码:523 / 526
页数:4
相关论文
共 50 条
  • [21] EMERGING DIFFERENCES BETWEEN 5-HT3 RECEPTOR ANTAGONISTS
    MARR, HE
    DAVEY, PT
    BARTLETT, AJ
    [J]. ANTI-CANCER DRUGS, 1991, 2 (06) : 513 - 518
  • [22] DEVELOPMENT OF HIGH-AFFINITY 5-HT3 RECEPTOR ANTAGONISTS .2. 2 NOVEL TRICYCLIC BENZAMIDES
    YOUSSEFYEH, RD
    CAMPBELL, HF
    AIREY, JE
    KLEIN, S
    SCHNAPPER, M
    POWERS, M
    WOODWARD, R
    RODRIGUEZ, W
    GOLEC, S
    STUDT, W
    DODSON, SA
    FITZPATRICK, LR
    PENDLEY, CE
    MARTIN, GE
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (05) : 903 - 911
  • [23] Preclinical and clinical pharmacology of the 5-HT3 receptor antagonists
    Wolf, H
    [J]. SCANDINAVIAN JOURNAL OF RHEUMATOLOGY, 2000, 29 : 37 - 45
  • [24] Current experience with 5-HT3 receptor antagonists in fibromyalgia
    Späth, M
    [J]. RHEUMATIC DISEASE CLINICS OF NORTH AMERICA, 2002, 28 (02) : 319 - +
  • [25] Spectrum of use and tolerability of 5-HT3 receptor antagonists
    Haus, U
    Späth, M
    Färber, L
    [J]. SCANDINAVIAN JOURNAL OF RHEUMATOLOGY, 2004, 33 : 12 - 18
  • [26] THE ECONOMIC-IMPACT OF 5-HT3 RECEPTOR ANTAGONISTS
    CUNNINGHAM, K
    HIRSCH, J
    FREEMAN, A
    [J]. EUROPEAN JOURNAL OF CANCER, 1993, 29A (06) : 930 - 930
  • [27] 5-HT3 receptor antagonists for the treatment of nausea/vomiting
    Smith, Howard S.
    Cox, Lorraine R.
    Smith, Eric J.
    [J]. ANNALS OF PALLIATIVE MEDICINE, 2012, 1 (02) : 115 - 120
  • [28] Novel 5-hydroxytryptamine (5-HT3) receptor antagonists .1. Synthesis and structure-activity relationships of conformationally restricted fused imidazole derivatives
    Ohta, M
    Suzuki, T
    Koide, T
    Matsuhisa, A
    Furuya, T
    Miyata, K
    Yanagisawa, I
    [J]. CHEMICAL & PHARMACEUTICAL BULLETIN, 1996, 44 (05) : 991 - 999
  • [29] 5-HT3 ANTAGONISTS AND EMESIS
    不详
    [J]. BRITISH JOURNAL OF HOSPITAL MEDICINE, 1990, 44 (04): : 293 - 293
  • [30] Conformationally restricted tryptamine sulfonamides as novel and selective 5-HT6 receptor antagonists
    Konda, Jagadishbabu
    Kambhampati, Rama Sastry
    Kothmirkar, Prabhakar
    Bandyala, Trinath Reddy
    Yarra, Sivasekhar N. K.
    Arepalli, Sobhanadri
    Rasheed, M. Abdul
    Shinde, Anil K.
    Nirogi, Ramakrishna
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2009, 237