新型取代吡咯烷是高亲和力组胺 H3 受体拮抗剂。
Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.
机构信息
Johnson & Johnson Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, United States.
出版信息
Bioorg Med Chem Lett. 2010 May 1;20(9):2755-60. doi: 10.1016/j.bmcl.2010.03.071. Epub 2010 Mar 20.
Pre-clinical characterization of novel substituted pyrrolidines that are high affinity histamine H(3) receptor antagonists is described. These compounds efficiently penetrate the CNS and occupy the histamine H(3) receptor in rat brain following oral administration. One compound, (2S,4R)-1-[2-(4-cyclobutyl-[1,4]diazepane-1-carbonyl)-4-(3-fluoro-phenoxy)-pyrrolidin-1-yl]-ethanone, was extensively profiled and shows promise as a potential clinical candidate.
描述了新型取代吡咯烷类化合物的临床前特征，这些化合物是高亲和力的组胺 H（3）受体拮抗剂。这些化合物经口服给药后，能够有效地穿透中枢神经系统并占据大鼠脑中的组胺 H（3）受体。一种化合物，（2S,4R）-1-[2-（4-环丁基-[1,4]二氮杂环庚烷-1-羰基）-4-（3-氟-苯氧基）-吡咯烷-1-基]-乙酮，经过了广泛的分析，有望成为一种潜在的临床候选药物。
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