作者:Katarzyna Kieć-Kononowicz、Xavier Ligneau、Holger Stark、Jean-Charles Schwartz、Walter Schunack
DOI:10.1002/ardp.19953280509
日期:——
structure‐activity relationships among histamine H3‐receptor antagonists the imidazole ring of known H3‐receptor antagonists was replaced by different heteroaromatic ring systems. Thus, azines and diazines with ether (6–13) and carbamate (15–24) moieties as functional groups were synthesized. The obtained compounds did not show significant H3‐receptor antagonist activity in vitro (rat brain cortex) or
为了寻找组胺 H3 受体拮抗剂之间的构效关系,已知 H3 受体拮抗剂的咪唑环被不同的杂芳环系统取代。因此,合成了具有醚(6-13)和氨基甲酸酯(15-24)部分作为官能团的吖嗪和二嗪。所得化合物在体外(大鼠脑皮层)或体内(小鼠脑)中均未显示出显着的 H3-受体拮抗剂活性。还筛选了新化合物对离体的豚鼠回肠的 H1-受体拮抗剂活性和对离体的自发搏动的豚鼠右心房的 H2-受体拮抗剂活性。这些物质对组胺受体 H1 和 H2 仅表现出微弱的拮抗活性。