Łazewska D, Kieć-Kononowicz K, Pertz H H, Elz S, Stark H, Schunack W
Department of Chemical Technology of Drugs, Medical College, Jagiellonian University, Kraków, Poland.
Pharmazie. 2002 Dec;57(12):791-5.
Recently novel leads for histamine H3 receptor antagonists of the non-imidazole type have been described. As a continuation of this research eleven new carbamate derivatives possessing an additional ether functionality were prepared. The compounds were evaluated in vitro for their antagonist activity on isolated organs of guinea-pig (GP) H3 as well as H2, H1, and M3 receptors, respectively. All compounds investigated possessed moderate antagonist affinities at guinea-pig histamine H3 receptors (pA2 6.11-6.76). An ether functionality introduced in different places of the lipophilic part of carbamates differently influenced activity and selectivity toward H3, M3, and other histamine receptors tested.
最近已报道了新型非咪唑类组胺H3受体拮抗剂的先导化合物。作为该研究的延续，制备了11种具有额外醚官能团的新型氨基甲酸酯衍生物。分别在体外评估了这些化合物对豚鼠（GP）H3以及H2、H1和M3受体的离体器官的拮抗活性。所有研究的化合物在豚鼠组胺H3受体上均具有中等拮抗亲和力（pA2为6.11 - 6.76）。在氨基甲酸酯亲脂部分的不同位置引入的醚官能团对H3、M3和其他受试组胺受体的活性和选择性有不同影响。
