THE SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF ENANTIOMERICALLY PURE HYDROXYLATED OXOTREMORINE DERIVATIVES

被引:11
|
作者
TRYBULSKI, EJ
KRAMSS, RH
MANGANO, RM
BRABANDER, HJ
FRANCISCO, G
机构
[1] Medical Research Division, American Cyanamid Co., Lederle Labs., Pearl River
关键词
D O I
10.1016/S0960-894X(00)80539-9
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and radioligand binding data of optically active hydroxylated oxotremorine derivatives are described. There are significant pharmacological differences between the enantiomers. most notably at the 3- and 4-position of the pyrrolidinone ring. In addition, there appears to be one side of the pyrrolidinone ring that accommodates substitutents better than the other (facial selectivity).
引用
收藏
页码:827 / 832
页数:6
相关论文
共 50 条
  • [31] STRUCTURE-ACTIVITY-RELATIONSHIPS
    FERSHT, AR
    PROTEIN ENGINEERING, 1987, 1 (03): : 233 - 233
  • [32] STRUCTURE-ACTIVITY-RELATIONSHIPS
    ARCOS, JC
    ENVIRONMENTAL SCIENCE & TECHNOLOGY, 1987, 21 (08) : 743 - 745
  • [33] NEW THIAZOLO[3,2-A]PYRIMIDINE DERIVATIVES, SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS
    JEANNEAUNICOLLE, E
    BENOITGUYOD, M
    NAMIL, A
    LECLERC, G
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 1992, 27 (02) : 115 - 120
  • [34] SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF NAPHTHALENE-SUBSTITUTED DERIVATIVES OF THE ALLYLAMINE ANTIMYCOTIC TERBINAFINE
    NUSSBAUMER, P
    DORFSTATTER, G
    LEITNER, I
    MRAZ, K
    VYPLEL, H
    STUTZ, A
    JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (19) : 2810 - 2816
  • [35] STRUCTURE-ACTIVITY-RELATIONSHIPS FOR THE AUXIN-LIKE ACTIVITY OF BENZOTRIAZOLE DERIVATIVES
    SPARATORE, F
    LAROTONDA, MI
    CALIENDO, G
    NOVELLINO, E
    SILIPO, C
    VITTORIA, A
    FARMACO-EDIZIONE SCIENTIFICA, 1988, 43 (02): : 141 - 151
  • [36] CYPROHEPTADINE ANALOGS - SYNTHESIS, ANTISEROTONINERGIC ACTIVITY, AND STRUCTURE-ACTIVITY-RELATIONSHIPS
    LOZA, MI
    SANZ, F
    CADAVID, MI
    HONRUBIA, M
    ORALLO, F
    FONTENLA, JA
    CALLEJA, JM
    DOT, T
    MANAUT, F
    CID, MM
    DOMINGUEZ, R
    SEIJAS, JA
    VILLAVERDE, MC
    JOURNAL OF PHARMACEUTICAL SCIENCES, 1993, 82 (11) : 1090 - 1093
  • [37] PROGESTERONE DERIVATIVES THAT BIND TO THE DIGITALIS RECEPTOR - STRUCTURE-ACTIVITY-RELATIONSHIPS
    KIM, RS
    LABELLA, FS
    ZUNZA, H
    ZUNZA, F
    TEMPLETON, JF
    MOLECULAR PHARMACOLOGY, 1980, 18 (03) : 402 - 405
  • [38] STUDIES ON THE QUANTITATIVE STRUCTURE-ACTIVITY-RELATIONSHIPS IN PYRAZINE CARBOTHIOAMIDE DERIVATIVES
    KALISZAN, R
    FOKS, H
    JANOWIEC, M
    POLISH JOURNAL OF PHARMACOLOGY AND PHARMACY, 1978, 30 (04): : 579 - 583
  • [39] STRUCTURE-ACTIVITY-RELATIONSHIPS OF BDB AND ITS MONOMETHYL AND DIMETHYL DERIVATIVES
    BRONSON, ME
    JIANG, W
    DERUITER, J
    CLARK, CR
    PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, 1995, 51 (2-3) : 477 - 479
  • [40] STRUCTURE-ACTIVITY-RELATIONSHIPS OF ALKYLXANTHINE DERIVATIVES AT RAT A(3)-RECEPTORS
    KIM, HO
    JI, XD
    OLAH, ME
    STILES, GL
    JACOBSON, KA
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1994, 208 : 206 - MEDI