Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists

被引：48

作者：

Ursini, A

Capelli, AM

Carr, RAE

Cassarà, P

Corsi, M

Curcuruto, O

Curotto, G

Dal Cin, M

Davalli, S

Donati, D

Feriani, A

Finch, H

Finizia, G

Gaviraghi, G

Marien, M

Pentassuglia, G

Polinelli, S

Ratti, E

Reggiani, A

Tarzia, G

Tedesco, G

Tranquillini, ME

Trist, DG

Van Amsterdam, FTM

机构：

[1] Glaxo Wellcome Inc, Med Res Ctr, I-37135 Verona, Italy

[2] Glaxo Wellcome Inc, Med Res Ctr, Stevenage SG1 2NY, Herts, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2000年 / 43卷 / 20期

关键词：

D O I：

10.1021/jm990967h

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 5-phenyl-3-ureidobenzodiazepine-2,4-diones was synthesized and evaluated as cholecystokinin-B (CCK-B) receptor antagonists. Structure-activity relationship (SAR) studies revealed the importance of the N-1 substituent for potent and selective CCK-B affinity. Addition of substituents at the urea side chain provided in some cases more potent compounds. Moreover the introduction of bulky substituents such as adamantylmethyl at; N-1 and resolution of the racemic ureas resulted in our lead compound GV150013.

引用

页码：3596 / 3613

页数：18

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