Synthesis, structure-activity relationships, and anxiolytic activity of 7-aryl-6,7-dihydroimidazoimidazole corticotropin-releasing factor 1 receptor antagonists

被引：17

作者：

Han, XJ

Michne, JA

Pin, SS

Burris, KD

Balanda, LA

Fung, LK

Fiedler, T

Browman, KE

Taber, MT

Zhang, J

Dubowchik, GM

机构：

[1] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA

[2] AstraZeneca R&D Boston, Infect Discovery, Waltham, MA 02451 USA

[3] Palatin Technol Inc, Cranbury, NJ 08512 USA

[4] Neurogen Corp, Branford, CT 06405 USA

[5] Abbott Labs, Dept R4N5, Abbott Pk, IL 60064 USA

[6] Sanofi Aventis, Bridgewater, NJ 08807 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 17期

关键词：

corticotropin-releasing factor 1 receptor antagonists; SAR; anxiolytic activity; mouse canopy model;

D O I：

10.1016/j.bmcl.2005.05.117

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

7-Aryl-6,7-dihydroimidazoimidazoles represent a novel series of high-affinity corticotropin-releasing factor I receptor antagonists. Here, we report their synthesis and SAR as well as behavioral activity of two exemplary compounds, 7b and 7k, in a mouse canopy model of anxiety. (c) 2005 Elsevier Ltd. All rights reserved.

引用

收藏

页码：3870 / 3873

页数：4

相关论文

共 20 条

[1]

Anisimova VA, 1999, PHARM CHEM J, V33, P361, DOI DOI 10.1007/BF02508707

[2] SEMINARS IN MEDICINE OF THE BETH-ISRAEL-HOSPITAL, BOSTON - THE HYPOTHALAMIC-PITUITARY-ADRENAL AXIS AND IMMUNE-MEDIATED INFLAMMATION [J].

CHROUSOS, GP .

NEW ENGLAND JOURNAL OF MEDICINE, 1995, 332 (20) :1351-1362

[3] Functional corticotropin-releasing factor receptors in human neuroblastoma cells [J].

Dieterich, KD ;

DeSouza, EB .

BRAIN RESEARCH, 1996, 733 (01) :113-118

[4] 2-arylaminothiazoles as high-affinity corticotropin-releasing factor 1 receptor (CRF1R) antagonists:: Synthesis, binding studies and behavioral efficacy [J].

Dubowchik, GM ;

Michne, JA ;

Zuev, D ;

Schwartz, W ;

Scola, PM ;

James, CA ;

Ruediger, EH ;

Pin, SS ;

Burris, KD ;

Balanda, LA ;

Gao, Q ;

Wu, DD ;

Fung, L ;

Fiedler, T ;

Browman, KE ;

Taber, MT ;

Zhang, J .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2003, 13 (22) :3997-4000

[5] Corticotropin releasing factor (CRF) receptor modulators: Progress and opportunities for new therapeutic agents [J].

Gilligan, PJ ;

Robertson, DW ;

Zaczek, R .

JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (09) :1641-1660

[6]

GILLIGAN PJ, 2000, 219 ACS NAT M SAN FR

[7] Behavioural and pharmacological characterisation of the canopy stretched attend posture test as a model of anxiety in mice and rats [J].

Grewal, SS ;

Shepherd, JK ;

Bill, DJ ;

Fletcher, A ;

Dourish, CT .

PSYCHOPHARMACOLOGY, 1997, 133 (01) :29-38

[8]

Grigoriadis Dimitri E., 2001, Current Medicinal Chemistry - Central Nervous System Agents, V1, P63, DOI 10.2174/1568015013358734

[9] International union of pharmacology. XXXVI. Current status of the nomenclature for receptors for corticotropin-releasing factor and their ligands [J].

Hauger, RL ;

Grigoriadis, DE ;

Dallman, MF ;

Plotsky, PM ;

Vale, WW ;

Dautzenberg, FM .

PHARMACOLOGICAL REVIEWS, 2003, 55 (01) :21-26

[10] Phenylimidazolidin-2-one derivatives as selective 5-HT3 receptor antagonists and refinement of the pharmacophore model for 5-HT3 receptor binding [J].

Heidempergher, F ;

Pillan, A ;

Pinciroli, V ;

Vaghi, F ;

Arrigoni, C ;

Bolis, G ;

Caccia, C ;

Dho, L ;

McArthur, R ;

Varasi, M .

JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (21) :3369-3380