SAR of novel biarylmethylamine dopamine D4 receptor ligands

被引:19
作者
Arlt, M [1 ]
Böttcher, H
Riethmüller, A
Schneider, G
Bartoszyk, GD
Greiner, H
Seyfried, CA
机构
[1] Merck KGaA, Med Chem ZNS, D-64271 Darmstadt, Germany
[2] Merck KGaA, BioMed Fo ZNS, D-64271 Darmstadt, Germany
关键词
D O I
10.1016/S0960-894X(98)00361-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
SAR for a novel series of dopamine Dq receptor ligands is shown. Very selective, highly potent compounds like 1-(2-pyrimidinyl)-4-(3-(3-thienyl)-benzyl)-piperazine (5f) and 2-(4-(1-fluorenylmethyl)-1-piperazinyl)-pyrimidine (8c) were obtained. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2033 / 2038
页数:6
相关论文
共 15 条
  • [1] Arlt M., 1997, Society for Neuroscience Abstracts, V23, P685
  • [2] N-(substituted-phenyl) piperazines: Antagonists with high binding and functional selectivity for dopamine D-4 receptors
    Boyfield, I
    Coldwell, MC
    Hadley, MS
    Healy, MAM
    Johns, A
    Nash, DJ
    Riley, GJ
    Scott, EE
    Smith, SA
    Stemp, G
    Wilson, K
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1996, 6 (11) : 1227 - 1232
  • [3] Design and synthesis of 2-naphthoate esters as selective dopamine D-4 antagonists
    Boyfield, I
    Brown, TH
    Coldwell, MC
    Cooper, DG
    Hadley, MS
    Hagan, JJ
    Healy, MA
    Johns, A
    King, RJ
    Middlemiss, DN
    Nash, DJ
    Riley, GJ
    Scott, EE
    Smith, SA
    Stemp, G
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (10) : 1946 - 1948
  • [4] Substituted [(4-phenylpiperazinyl)methyl]benzamides: Selective dopamine D-4 agonists
    Glase, SA
    Akunne, HC
    Georgic, LM
    Heffner, TG
    MacKenzie, RG
    Manley, PJ
    Pugsley, TA
    Wise, LD
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (12) : 1771 - 1772
  • [5] HADLEY MS, 1996, MED REV, V16, P527
  • [6] Hoffman D. C., 1995, Society for Neuroscience Abstracts, V21, P469
  • [7] SYNTHESIS OF SOME 4-SUBSTITUTED AND 4,6-DISUBSTITUTED DIBENZOTHIOPHENES
    KATRITZKY, AR
    PERUMAL, S
    [J]. JOURNAL OF HETEROCYCLIC CHEMISTRY, 1990, 27 (06) : 1737 - 1740
  • [8] PREPARATION AND REACTIONS OF POLYFUNCTIONAL ORGANOZINC REAGENTS IN ORGANIC-SYNTHESIS
    KNOCHEL, P
    SINGER, RD
    [J]. CHEMICAL REVIEWS, 1993, 93 (06) : 2117 - 2188
  • [9] Kramer MS, 1997, ARCH GEN PSYCHIAT, V54, P567
  • [10] 3-[[4-(4-chlorophenyl)piperazin-1-yl]methyl]-1H-pyrrolo[2,3-b]pyridine: An antagonist with high affinity and selectivity for the human dopamine D-4 receptor
    Kulagowski, JJ
    Broughton, HB
    Curtis, NR
    Mawer, IM
    Ridgill, MP
    Baker, R
    Emms, F
    Freedman, SB
    Marwood, R
    Patel, S
    Patel, S
    Ragan, CI
    Leeson, PD
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (10) : 1941 - 1942