Parallel solution- and solid-phase synthesis of spiropyrrolo-pyrroles as novel neurokinin receptor ligands

被引：27

作者：

Bleicher, KH ^{[1
]}

Wüthrich, Y ^{[1
]}

Adam, G ^{[1
]}

Hoffmann, T ^{[1
]}

Sleight, AJ ^{[1
]}

机构：

[1] F Hoffmann La Roche & Co Ltd, Pharma Res, CH-4070 Basel, Switzerland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 21期

关键词：

D O I：

10.1016/S0960-894X(02)00659-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The combination of a 3,5-bis(trifluoromethyl)phenyl needle with the spiropyrrolo-pyrrole motive as a privileged GPCR scaffold was the basis for designing a focused combinatorial library targeted towards the neurokinin-1 receptor. A solution- and solid-phase method is described and binding affinities of representative compounds are presented. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：3073 / 3076

页数：4

共 9 条

[1] Structural characterization and binding sites of G-protein-coupled receptors
BeckSickinger, AG
[J]. DRUG DISCOVERY TODAY, 1996, 1 (12) : 502 - 513
[2] Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands
Bleicher, KH
Wüthrich, Y
De Boni, M
Kolczewski, S
Hoffmann, T
Sleight, AJ
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (18) : 2519 - 2522
[3] Novel inhibitors of DNA gyrase: 3D structure based biased needle screening, hit validation by biophysical methods, and 3D guided optimization. A promising alternative to random screening
Boehm, HJ
Boehringer, M
Bur, D
Gmuender, H
Huber, W
Klaus, W
Kostrewa, D
Kuehne, H
Luebbers, T
Meunier-Keller, N
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (14) : 2664 - 2674
[4] Dautzenberg F, 1999, Eur Pat Appl, Patent No. 0963987
[5] New 4-point pharmacophore method for molecular similarity and diversity applications: Overview of the method and applications, including a novel approach to the design of combinatorial libraries containing privileged substructures
Mason, JS
Morize, I
Menard, PR
Cheney, DL
Hulme, C
Labaudiniere, RF
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (17) : 3251 - 3264
[6] Privileged structures - An update
Patchett, AA
Nargund, RP
[J]. ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 35, 2000, 35 : 289 - 298
[7] ORPHANIN-FQ - A NEUROPEPTIDE THAT ACTIVATES AN OPIOID-LIKE G-PROTEIN-COUPLED RECEPTOR
REINSCHEID, RK
NOTHACKER, HP
BOURSON, A
ARDATI, A
HENNINGSEN, RA
BUNZOW, JR
GRANDY, DK
LANGEN, H
MONSMA, FJ
CIVELLI, O
[J]. SCIENCE, 1995, 270 (5237) : 792 - 794
[8] Neurokinin receptor antagonists
Seward, EM
Swain, CJ
[J]. EXPERT OPINION ON THERAPEUTIC PATENTS, 1999, 9 (05) : 571 - 582
[9] SIMPLE GENERATION OF ESTER-STABILIZED AZOMETHINE YLIDES FROM 2-AMINO ESTERS AND CARBONYL-COMPOUNDS - STEREOCHEMISTRY OF THEIR CYCLOADDITIONS
TSUGE, O
KANEMASA, S
OHE, M
YOROZU, K
TAKENAKA, S
UENO, K
[J]. BULLETIN OF THE CHEMICAL SOCIETY OF JAPAN, 1987, 60 (11) : 4067 - 4078

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