Successful bridging from a peptide to a non peptide antagonist at the human tachykinin NK-2 receptor

被引：11

作者：

Altamura, M ^{[1
]}

Canfarini, F ^{[1
]}

Catalioto, RM ^{[1
]}

Guidi, A ^{[1
]}

Pasqui, F ^{[1
]}

Renzetti, AR ^{[1
]}

Triolo, A ^{[1
]}

Maggi, CA ^{[1
]}

机构：

[1] Menarini Ric SpA, I-50131 Florence, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(02)00539-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Non peptide products have been found to show nanomolar binding and functional affinities at the human tachykinin NK-2 receptor. The new antagonists do not possess stereogenic centers and their thermal behaviour in solution is featured by a peculiar set of conformational stereoisomers. A macroscopic viewpoint is preferentially adopted to rationalize the obtained results. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

收藏

页码：2945 / 2948

页数：4

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共 28 条

[21] DESIGN AND STRUCTURE OF A NOVEL NEUROKININ A RECEPTOR ANTAGONIST CYCLO(-MET(1)-ASP(2)-TRP(3)-PHE(4)-DAP(5)-LEU(6)-)CYCLO(2-BETA-5-BETA) [J].

PAVONE, V ;

LOMBARDI, A ;

NASTRI, F ;

SAVIANO, M ;

MAGLIO, O ;

DAURIA, G ;

QUARTARA, L ;

MAGGI, CA ;

PEDONE, C .

JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 2, 1995, (05) :987-993

[22] PEPTIDE-BASED TACHYKININ NK2 RECEPTOR ANTAGONISTS [J].

QUARTARA, L ;

ROVERO, P ;

MAGGI, CA .

MEDICINAL RESEARCH REVIEWS, 1995, 15 (02) :139-155

[23] Vicinal diamides as lanthanide complexers with two conformational states of different dipole moments - Elements for new molecular switches [J].

Schneider, HJ ;

Kasper, C ;

Palyulin, V ;

Samoshin, VV .

SUPRAMOLECULAR CHEMISTRY, 1997, 8 (03) :225-229

[24] NEW SPIROPIPERIDINES AS POTENT AND SELECTIVE NONPEPTIDE TACHYKININ NK2 RECEPTOR ANTAGONISTS [J].

SMITH, PW ;

COOPER, AWJ ;

BELL, R ;

BERESFORD, IJM ;

GORE, PM ;

MCELROY, AB ;

PRITCHARD, JM ;

SAEZ, V ;

TAYLOR, NR ;

SHELDRICK, RLG ;

WARD, P .

JOURNAL OF MEDICINAL CHEMISTRY, 1995, 38 (19) :3772-3779

[25] PA2 AND RECEPTOR DIFFERENTIATION - STATISTICAL-ANALYSIS OF COMPETITIVE ANTAGONISM [J].

TALLARIDA, RJ ;

COWAN, A ;

ADLER, MW .

LIFE SCIENCES, 1979, 25 (08) :637-654

[26] Regio- and stereoselective cycloadditions of cyclic nitrones to maleic diamide forced in a peptide: Synthesis of potent ligands of human NK-2 receptor [J].

Valenza, S ;

Cordero, FM ;

Brandi, A ;

Guidi, A ;

Altamura, M ;

Giolitti, A ;

Giuntini, F ;

Pasqui, F ;

Renzetti, AR ;

Maggi, CA .

JOURNAL OF ORGANIC CHEMISTRY, 2000, 65 (13) :4003-4008

[27] The effect of the NK2 tachykinin receptor antagonist SR 48968 (saredutant) on neurokinin A-induced bronchoconstriction in asthmatics [J].

Van Schoor, J ;

Joos, GF ;

Chasson, BL ;

Brouard, RJ ;

Pauwels, RA .

EUROPEAN RESPIRATORY JOURNAL, 1998, 12 (01) :17-23

[28] ALKYL-OXYGEN CLEAVAGE OF AN ESTER BY PRIMARY AND SECONDARY AMINES [J].

ZAUGG, HE ;

HELGREN, PF ;

SCHAEFER, AD .

JOURNAL OF ORGANIC CHEMISTRY, 1963, 28 (10) :2617-&