Ali S M, Tedford C E, Gregory R, Yates S L, Phillips J G
Gliatech Inc., Cleveland, Ohio 44122, USA.
Bioorg Med Chem Lett. 1998 May 19;8(10):1133-8. doi: 10.1016/s0960-894x(98)00181-4.
New histamine H3 receptor antagonists were developed using an acetylene moiety as a replacement for the amide-oxime functionality of verongamine 5. Optimization of receptor binding was performed by following aliphatic Topliss tree guidelines. These new H3 ligands demonstrate excellent blood-brain barrier penetration.
新型组胺H3受体拮抗剂是通过使用乙炔部分取代维隆胺5的酰胺肟官能团而开发的。通过遵循脂肪族托普利斯树指南进行受体结合的优化。这些新型H3配体显示出优异的血脑屏障穿透性。
