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首页> 外文期刊>Journal of Medicinal Chemistry >A Selective Human H_4-Receptor Agonist: (-)-2-Cyano-1-methyl-3-{(2R,5R)-5-[1H-imidazol-4(5)-yl]tetrahydrofuran-2-yl}methylguanidine
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A Selective Human H_4-Receptor Agonist: (-)-2-Cyano-1-methyl-3-{(2R,5R)-5-[1H-imidazol-4(5)-yl]tetrahydrofuran-2-yl}methylguanidine

机译:选择性人类H_4-受体激动剂:(-)-2-氰基-1-甲基-3-{(2R,5R)-5- [1H-咪唑-4(5)-基]四氢呋喃-2-基}甲基胍

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摘要

A series of 16 compounds related to chiral 4(5)-(5-aminomethyltetrahydrofuran-2-yl)imidazoles (1) have been designed, synthesized, and examined in vitro by radioligand displacement studies and functional assays for both the human H_3- and H_4-receptors expressed in SK-N-MC cells. Among them, the (2S,5S)-isomer 1d of amino compounds showed approximately 300-fold higher selectivity at the H_3-receptor than the H4-receptor. On the other hand, (2R,5S)- and (2R,5R)-cyanoguanidines 3b and 3c, in which the amino group of the compounds 1b and 1c was substituted by the cyanoguanidino moiety, bound to the H_4-receptor with a pEC_(50) value of 6.65 and 7.11, respectively, and had >40-fold selectivities over the H_3-receptor. As such, 3b and 3c are the first selective H_4 receptor agonists.
机译:已通过放射配体置换研究和针对人H_3和H_3的功能测定体外设计,合成和检查了一系列与手性4(5)-(5-氨基甲基四氢呋喃-2-基)咪唑(1)相关的16种化合物在SK-N-MC细胞中表达的H_4-受体。其中,氨基化合物的(2S,5S)异构体1d在H_3受体上的选择性比H4受体高约300倍。另一方面,化合物(1b和1c的氨基被氰基胍基部分取代)的(2R,5S)-和(2R,5R)-氰基胍3b和3c通过pEC_与H_4-受体结合。 (50)的值分别为6.65和7.11,并且具有比H_3受体高40倍以上的选择性。这样,3b和3c是第一选择性H_4受体激动剂。

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