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

Authors
CHAMBERS MS HOBBS SC GRAHAM MI WATT AP FLETCHER SR BAKER R FREEDMAN SB PATEL S SMITH AJ MATASSA VG
Citation
Ms. Chambers et al., POTENT, SELECTIVE, WATER-SOLUBLE BENZODIAZEPINE-BASED CCKB RECEPTOR ANTAGONISTS THAT CONTAIN LIPOPHILIC CARBOXYLATE SURROGATES, Bioorganic & medicinal chemistry letters, 5(20), 1995, pp. 2303-2308
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
20
Year of publication
1995
Pages
2303 - 2308
Database
ISI
SICI code
0960-894X(1995)5:20<2303:PSWBCR>2.0.ZU;2-E
Abstract
Acylsulphonamide analogues of the meta-tolylurea L-708,474 have been s ynthesised and evaluated as CCKB receptor antagonists. Such derivative s retain very high affinity and subtype selectivity for the CCKB recep tor, and have good aqueous solubility. The ortho-tolyl acylsulphonamid e L-736,309 is orally bioavailable and brain penetrant in rat.