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新型 N-取代-N-[ω-(ω-苯氧基烷基亚基哌嗪-1-基)烷基]胍类化合物的合成及初步药理学研究作为非咪唑组胺 H（3）拮抗剂。

Synthesis and preliminary pharmacological investigation of new N-substituted-N-[ω-(ω-phenoxy-alkylpiperazin-1-yl)alkyl]guanidines as non-imidazole histamine H(3) antagonists.

机构信息

Department of Synthesis and Technology of Drugs, Medical University, Łódź, Poland.

出版信息

Arch Pharm (Weinheim). 2012 Jun;345(6):431-43. doi: 10.1002/ardp.201100428. Epub 2012 Mar 13.

DOI:10.1002/ardp.201100428
PMID:22415744
Abstract

Novel, potent non-imidazole histamine H(3) receptor antagonists were prepared. Detailed structure-activity studies revealed that N-(4-trifluoromethylbenzyl)-N-[4-(7-phenoxyheptylpiperazin-1-yl)butyl]guanidine (pA(2)  = 8.49 ± 0.05), 1h, and N-(4-nitrobenzyl)-N-[4-(7-phenoxyheptylpiperazin-1-yl)butyl]guanidine (pA(2)  = 8.43 ± 0.05), 1l, exhibit high affinity for the H(3) histamine receptor. The most potent antagonists in this series, 1e, 1h, and 1l, were also in vitro tested as H(1) receptor antagonists, showing weak H(1) -antagonistic activity with pA(2)  = 6.70 ± 0.09, pA(2)  = 6.46 ± 0.09, and pA(2)  = 6.65 ± 0.11, respectively.

摘要

新型强效非咪唑类组胺 H（3）受体拮抗剂被制备。详细的构效关系研究表明，N-（4-三氟甲基苄基）-N-[4-（7-苯氧基庚基哌嗪-1-基）丁基]胍（pA（2）=8.49±0.05），1h 和 N-（4-硝基苄基）-N-[4-（7-苯氧基庚基哌嗪-1-基）丁基]胍（pA（2）=8.43±0.05），1l，对 H（3）组胺受体具有高亲和力。该系列中最有效的拮抗剂 1e、1h 和 1l 也作为 H（1）受体拮抗剂进行了体外测试，表现出较弱的 H（1）拮抗活性，pA（2）=6.70±0.09、pA（2）=6.46±0.09 和 pA（2）=6.65±0.11。

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