Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands

被引：19

作者：

Bleicher, KH ^{[1
]}

Wüthrich, Y ^{[1
]}

De Boni, M ^{[1
]}

Kolczewski, S ^{[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 / 18期

关键词：

D O I：

10.1016/S0960-894X(02)00488-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The combination of the 3,5-bis(trifluoromethyl)phenyl group with a spirohydantoin motive as a central scaffold was the basis for the design of a combinatorial library targeted towards the neurokinin-1 receptor. A solution-and solid-phase procedure is described and binding affinities of representative compounds presented. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：2519 / 2522

页数：4

共 15 条

[1] 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
[2] Angiotensin II receptor antagonists
Burnier, M
Brunner, HR
[J]. LANCET, 2000, 355 (9204) : 637 - 645
[3] Solid phase hydantoin synthesis: An efficient and direct conversion of Fmoc-protected dipeptides to hydantoins
Chong, PY
Petillo, PA
[J]. TETRAHEDRON LETTERS, 1999, 40 (13) : 2493 - 2496
[4] DEWITT SH, 1993, P NATL ACAD SCI USA, V90, P6900
[5] Modelling G-protein-coupled receptors for drug design
Flower, DR
[J]. BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON BIOMEMBRANES, 1999, 1422 (03): : 207 - 234
[6] Galley G., 2001, Patent No. [0194346A1, 0194346]
[7] Solid phase synthesis of hydantoin library using a novel cyclization and traceless cleavage step
Kim, SW
Ahn, SY
Koh, JS
Lee, JH
Ro, S
Cho, HY
[J]. TETRAHEDRON LETTERS, 1997, 38 (26) : 4603 - 4606
[8] Synthesis and antiviral activity evaluation of some new aminoadamantane derivatives .2.
Kolocouris, N
Kolocouris, A
Foscolos, GB
Fytas, G
Neyts, J
Padalko, E
Balzarini, J
Snoeck, R
Andrei, G
DeClercq, E
[J]. JOURNAL OF MEDICINAL CHEMISTRY, 1996, 39 (17) : 3307 - 3318
[9] Neurokinin receptor antagonists
Leroy, V
Mauser, P
Gao, ZL
Peet, NP
[J]. EXPERT OPINION ON INVESTIGATIONAL DRUGS, 2000, 9 (04) : 735 - 746
[10] 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

← 1 2 →