Wolin R, Connolly M, Afonso A, Hey J A, She H, Rivelli M A, Willams S M, West R E
Schering-Plough Research Institute, Department of Chemistry, Kenilworth, New Jersey 07033, USA.
Bioorg Med Chem Lett. 1998 Aug 18;8(16):2157-62. doi: 10.1016/s0960-894x(98)00379-5.
Sulfonamides derived from 4(5)-(omega-aminoalkyl)-1H-imidazoles containing chain lengths of three- to five-carbons were synthesized. Good to moderate H3 receptor binding affinities were observed for several butyl and pentyl homologs, whereas binding affinities were considerably weaker in the propyl series. Separation of the imidazole ring and the sulfonamide unit by a four- or five-carbon tether afforded potent H3 receptor antagonists.
合成了衍生自含有三至五个碳链长度的4(5)-(ω-氨基烷基)-1H-咪唑的磺胺类化合物。几种丁基和戊基同系物表现出良好至中等的H3受体结合亲和力，而丙基系列的结合亲和力则弱得多。通过四碳或五碳连接链将咪唑环和磺酰胺单元隔开可得到强效的H3受体拮抗剂。
