POTENT, SELECTIVE, WATER-SOLUBLE BENZODIAZEPINE-BASED CCKB RECEPTOR ANTAGONISTS THAT CONTAIN LIPOPHILIC CARBOXYLATE SURROGATES

被引：23

作者：

CHAMBERS, MS

HOBBS, SC

GRAHAM, MI

WATT, AP

FLETCHER, SR

BAKER, R

FREEDMAN, SB

PATEL, S

SMITH, AJ

MATASSA, VG

机构：

[1] Merck, Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex CM20 2QR, Terlings Park, Eastwick Road

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 20期

关键词：

D O I：

10.1016/0960-894X(95)00399-E

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Acylsulphonamide analogues of the meta-tolylurea L-708,474 have been synthesised and evaluated as CCKB receptor antagonists. Such derivatives retain very high affinity and subtype selectivity for the CCKB receptor, and have good aqueous solubility. The ortho-tolyl acylsulphonamide L-736,309 is orally bioavailable and brain penetrant in rat.

引用

页码：2303 / 2308

页数：6

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