DESIGN AND SYNTHESIS OF A PROTOTYPE MODEL ANTAGONIST OF TACHYKININ NK-2 RECEPTOR

被引:35
作者
HANESSIAN, S [1 ]
RONAN, B [1 ]
LAOUI, A [1 ]
机构
[1] RHONE POULENC RORER SA, CENT RES, CTR RECH VITRY ALFORTVILLE, F-94403 VITRY, FRANCE
关键词
D O I
10.1016/S0960-894X(01)80369-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A conformationally biased bicyclic lactam containing strategically placed hydrophobic groups was synthesized as a prototype model antagonist molecule of the NK-2 receptor.
引用
收藏
页码:1397 / 1400
页数:4
相关论文
共 51 条
[11]   THE TOTAL SYNTHESES OF THE ISODITYROSINE-DERIVED CYCLIC TRIPEPTIDES OF4949-III AND K-13 - DETERMINATION OF THE ABSOLUTE-CONFIGURATION OF K-13 [J].
EVANS, DA ;
ELLMAN, JA .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1989, 111 (03) :1063-1072
[12]   ELECTROPHILIC AZIDE TRANSFER TO CHIRAL ENOLATES - A GENERAL-APPROACH TO THE ASYMMETRIC-SYNTHESIS OF ALPHA-AMINO-ACIDS [J].
EVANS, DA ;
BRITTON, TC .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1987, 109 (22) :6881-6883
[13]   TOTAL SYNTHESIS OF THE ANGIOTENSIN-CONVERTING ENZYME INHIBITOR-A58365A - ON THE USE OF PYROGLUTAMATE AS A CHIRAL EDUCT [J].
FANG, FG ;
DANISHEFSKY, SJ .
TETRAHEDRON LETTERS, 1989, 30 (28) :3621-3624
[14]   SPANTIDE-II, AN EFFECTIVE TACHYKININ ANTAGONIST HAVING HIGH POTENCY AND NEGLIGIBLE NEUROTOXICITY [J].
FOLKERS, K ;
FENG, DM ;
ASANO, N ;
HAKANSON, R ;
WEISENFELDHALLIN, Z ;
LEANDER, S .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1990, 87 (12) :4833-4835
[15]   PEPTIDOMIMETICS FOR RECEPTOR LIGANDS DISCOVERY, DEVELOPMENT, AND MEDICAL PERSPECTIVES [J].
GIANNIS, A .
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 1993, 32 (09) :1244-1267
[16]  
GUILLAUME JM, 1993, 3RD ANN M NEUR CLUB
[17]   STUDIES ON NEUROKININ ANTAGONISTS .1. THE DESIGN OF NOVEL TRIPEPTIDES POSSESSING THE GLUTAMINYL-DEUTERIUM-TRYPTOPHYLPHENYLALANINE SEQUENCE AS SUBSTANCE-P ANTAGONISTS [J].
HAGIWARA, D ;
MIYAKE, H ;
MORIMOTO, H ;
MURAI, M ;
FUJII, T ;
MATSUO, M .
JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (11) :2015-2025
[18]   A FACILE SYNTHESIS OF THE NOVEL NEUROKININ-A ANTAGONIST SR-48968 [J].
HALE, JJ ;
FINKE, PE ;
MACCOSS, M .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1993, 3 (02) :319-322
[19]   HIGHLY STEREOCONTROLLED SYNTHESES OF 2,3-DISUBSTITUTED 1,4-BUTYROLACTONES USING IONIC AND FREE-RADICAL REACTIONS [J].
HANESSIAN, S ;
VANASSE, B ;
YANG, H ;
ALPEGIANI, M .
CANADIAN JOURNAL OF CHEMISTRY, 1993, 71 (09) :1407-1411
[20]   A NEW CLASS OF HIGH-AFFINITY LIGANDS FOR THE NEUROKININ-A NK2 RECEPTOR - PSI(CH2NR) REDUCED PEPTIDE-BOND ANALOGS OF NEUROKININ-A4-10 [J].
HARBESON, SL ;
SHATZER, SA ;
LE, TB ;
BUCK, SH .
JOURNAL OF MEDICINAL CHEMISTRY, 1992, 35 (21) :3949-3955