Non-imidazole histamine H3 ligands: part V. synthesis and preliminary pharmacological investigation of l-2-thiazol-4-yl- and l-2-thiazol-5-yl-(2-aminoethyl)-4-n-propylpiperazine derivatives

Roman Guryn; Marek Staszewski; Krzysztof Walczynski

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Non-imidazole histamine H3 ligands: part V. synthesis and preliminary pharmacological investigation of l-2-thiazol-4-yl- and l-2-thiazol-5-yl-(2-aminoethyl)-4-n-propylpiperazine derivatives

机译：非咪唑组胺H3配体：第五部分 L-2-噻唑-4-基-和L-2-噻唑-5-基-（2-氨基乙基）-4-正丙基哌嗪衍生物的合成和初步药理学研究

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Series of l-2-thiazol-4-yl-(2-aminoethyl)- and l-2-thiazol-5-yl-(2-aminoethyl)-4-n-propylpiperazine derivatives have been prepared and in vitro tested as H3-receptor antagonists (the electrically evoked contraction of the guinea-pig jejunum). It appeared that by comparison of homologous pairs, the l-2-thiazol-5-yl-(2-aminoethyl)-4-n-propylpipera-zines (3a,b and 4a-d) have much higher potency than their analogous l-2-thiazol-4-yl-(2-aminoethyl)-4-n-propylpiper-azines (2a-k). Based on the obtained results, we observed the 5-position of 2-methyl-2-R-aminoethyl substituents in the thiazole ring is favourable for histamine H3 receptor antagonist activity, whereas its presence in position 4 leads, almost in each case, to strong decrease of activity.

机译：已经制备了一系列 l-[2-噻唑-4-基-（2-氨基乙基）]和 l-[2-噻唑-5-基-（2-氨基乙基）]-4-正丙基哌嗪衍生物，并作为 H3 受体拮抗剂（豚鼠空肠的电诱发收缩）进行了体外测试。通过同源对的比较，l-[2-噻唑-5-基-（2-氨基乙基）]-4-正丙基胡椒嗪（3a，b和4a-d）的效力似乎比其类似的l-[2-噻唑-4-基-（2-氨基乙基）]-4-正丙基胡嗪嗪（2a-k）高得多。根据获得的结果，我们观察到噻唑环中 2-甲基-2-R-氨基乙基取代基的 5 位有利于组胺 H3 受体拮抗剂活性，而它在 4 位的存在几乎在每种情况下都会导致活性强烈降低。

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来源
《Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents》 |2013年第8期|3640-3652|共13页
作者
Roman Guryn; Marek Staszewski; Krzysztof Walczynski;
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Department of Synthesis and Technology of Drugs, Medical University, Muszyriskiego Street 1, 90-145;

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原文格式 PDF
正文语种英语
中图分类药学;
关键词
Histamine H3-receptor; H3-antagonists; l-2-thiazol-4-yl-(2-aminoethyl)-; l-2-thiazol-5-yl-(2-aminoethyl)-4-n-propylpiperazine derivatives;

机译：组胺H3受体;H3拮抗剂;L-[2-噻唑-4-基-（2-氨基乙基）]-;L-[2-噻唑-5-基-（2-氨基乙基）]-4-正丙基哌嗪衍生物;

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Non-imidazole histamine H3 ligands: part V. synthesis and preliminary pharmacological investigation of l-2-thiazol-4-yl- and l-2-thiazol-5-yl-(2-aminoethyl)-4-n-propylpiperazine derivatives

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