Il Farmaco p. 723 - 738 (2003)
Update date:2022-07-30
Topics:
Di Fabio, Romano
Micheli, Fabrizio
Baraldi, Davide
Bertani, Barbara
Conti, Nadia
Dal Forno, Giovanna
Feriani, Aldo
Donati, Daniele
Marchioro, Carla
Messeri, Tommaso
Missio, Andrea
Pasquarello, Alessandra
Pentassuglia, Giorgio
Pizzi, Domenica A.
Provera, Stefano
Quaglia, Anna M.
Sabbatini, Fabio M.
A series of benzoazepine derivatives, bearing suitable substituents at the C-3 position, was designed and evaluated by superimposition with the pharmacophore model of the glycine binding site. To fully explore the SAR of this class of compounds and to allow the preparation of new different compounds at the C-3 position, appropriate synthetic routes were set up. The benzoazepines were evaluated in terms of in vitro affinity using [ 3H]glycine binding assay and in vivo potency by inhibition of convulsions induced by N-methyl-D-aspartate (NMDA) in mice. This further analysis confirmed the preliminary results previously reported and that compound 27 is the most promising compound (Ki=32 nM, ED50=0.09 mg/kg, i.v.) in this series. Significant neuroprotective effect was observed after both pre- and post-ischaemia administration in the MCAo model. In particular, after post-ischaemia administration, it was found to be still effective when the administration was delayed up to 6 h after occlusion of the middle cerebral artery.
View Morewebsite:http://www.greenutra.cn
Contact:0086-411-39553357
Address:No. 7-1-1802, Huizhi Garden,Ocean Square,Dalian, 116033, China
Shanghai PotentPharm Science and Technology Co.,Ltd
Contact:86-021-51969655
Address:Unit B, Building 18, No.300, Chuantu Rd,Pudong District, Shanghai 201202, China
Contact:0086-29-89196322
Address:North of the Fifth Keji Road, Hi-Tech Industrial Zone, Xi'an City, Shaanxi Province, China
website:http://www.shochem.com
Contact:021-50800795
Address:No.1043, Halei Rd, Zhangjiang Hi-Tech Park, Shanghai, Postcode 201203, China
Shanghai Sunwise Chemical Co., Ltd
website:http://www.sunwisechem.com
Contact:86-021-33883180
Address:Room 10E, Building G, Westlink Center, No. 2337 Gudai Road, Minhang District, Shanghai, China PC: 201100
Doi:10.1021/ja00221a005
(1988)Doi:10.1039/j39690000301
(1969)Doi:10.1021/ja01623a044
(1955)Doi:10.1039/a808848i
(1999)Doi:10.1248/cpb.45.750
(1997)Doi:10.1002/hlca.19520350206
(1952)