Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists

被引：140

作者：

Wustrow, DJ ^{[1
]}

Capiris, T ^{[1
]}

Rubin, R ^{[1
]}

Knobelsdorf, JA ^{[1
]}

Akunne, H ^{[1
]}

Davis, MD ^{[1
]}

MacKenzie, R ^{[1
]}

Pugsley, TA ^{[1
]}

Zoski, KT ^{[1
]}

Heffner, TG ^{[1
]}

Wise, LD ^{[1
]}

机构：

[1] Parke Davis Pharmaceut Res, Ann Arbor, MI 48105 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(98)00372-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 3-phenylpyrazolo[1,5-a]pyrimidines was prepared and found to have affinity for the human CRF-1 receptor. The 3-dimensional structure of one of the most potent analogs in this series, 10d, was determined by X-ray crystallography and suggests the spatial requirements for potent CRF-1 receptor binding affinity in this series. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：2067 / 2070

页数：4

共 14 条

[1]

Chen C, 1996, J MED CHEM, V39, P4358

[2]

CHEN C, Patent No. 03510

[3]

CHEN C, Patent No. 29109

[4] Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: A centrally active corticotropin-releasing factor(1) receptor antagonist [J].

Chen, YL ;

Mansbach, RS ;

Winter, SM ;

Brooks, E ;

Collins, J ;

Corman, ML ;

Dunaiskis, AR ;

Faraci, WS ;

Gallaschun, RJ ;

Schmidt, A ;

Schulz, DW .

JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (11) :1749-1754

[5] Corticotrophin-releasing factor receptor antagonists [J].

Christos, TE ;

Arvanitis, A .

EXPERT OPINION ON THERAPEUTIC PATENTS, 1998, 8 (02) :143-152

[6] Corticotropin-releasing factor receptors: An overview [J].

Dieterich, KD ;

Lehnert, H ;

DeSouza, EB .

EXPERIMENTAL AND CLINICAL ENDOCRINOLOGY & DIABETES, 1997, 105 (02) :65-82

[7] CHEMISTRY OF PYRAZOLOPYRIMIDINES [J].

ELNAGDI, MH ;

ELMOGHAYAR, MRH ;

ELGEMEIE, GEH .

ADVANCES IN HETEROCYCLIC CHEMISTRY, 1987, 41 :319-376

[8] Corticotropin-releasing hormone (CRH) receptors and the discovery of selective non-peptide CRH1 antagonists [J].

Gilligan, PJ ;

Hartig, PR ;

Robertson, DW ;

Zaczek, R .

ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 32, 1997, 32 :41-50

[9] Corticotropin-releasing factor, stress, and depression [J].

Heit, S ;

Owens, MJ ;

Plotsky, P ;

Nemeroff, CB .

NEUROSCIENTIST, 1997, 3 (03) :186-194

[10]

Julian P. J., 1943, ORG SYNTH, VII, P487

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