8,8-二甲基[1,6]萘啶作为潜在抗惊厥剂的设计

The design of 8,8-dimethyl[1,6]naphthyridines as potential anticonvulsant agents.

作者信息

Austin Nigel E, Hadley Michael S, Harling John D, Harrington Frank P, Macdonald Gregor J, Mitchell Darren J, Riley Graham J, Stean Tania O, Stemp Geoffrey, Stratton Sharon C, Thompson Mervyn, Upton Neil

机构信息

Neurology & GI Centre of Excellence for Drug Discovery, GlaxoSmithKline Research & Development Limited, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.

出版信息

Bioorg Med Chem Lett. 2003 May 19;13(10):1627-9. doi: 10.1016/s0960-894x(03)00288-9.

DOI:10.1016/s0960-894x(03)00288-9

PMID:12729628

Abstract

Starting from a series of 7-linked tetrahydroisoquinoline derivatives, as exemplified by SB-270664, a new series of 8,8-dimethylnaphthyridine compounds has been identified. SAR studies around these attractive leads have provided compounds such as 12 which display excellent anticonvulsant activity and an encouraging pharmacokinetic profile in vivo.

摘要

从一系列以SB-270664为代表的7-连接四氢异喹啉衍生物出发，已鉴定出一系列新的8,8-二甲基萘啶化合物。围绕这些有吸引力的先导化合物进行的构效关系研究已得到了如化合物12等，其在体内表现出优异的抗惊厥活性和令人鼓舞的药代动力学特征。