林文清, 蔡纯一, 龚康孙, 吴, 勇, 龙, 翥, 罗晓星, 杨, 力, 李景峰, 姚秀娟. N-(4-甲氧羰基-4-邻苯二甲酰亚氨基丁酰基)-N-取代甘氨酸、脯氨酸和焦谷氨酸的合成J. 药学学报, 1994, 29(5): 346-354.
引用本文: 林文清, 蔡纯一, 龚康孙, 吴, 勇, 龙, 翥, 罗晓星, 杨, 力, 李景峰, 姚秀娟. N-(4-甲氧羰基-4-邻苯二甲酰亚氨基丁酰基)-N-取代甘氨酸、脯氨酸和焦谷氨酸的合成J. 药学学报, 1994, 29(5): 346-354.
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WQ Lin, CY Cai, KS Gong, Y Wu, Z Long, XX Luo’, L Yang’, JF Li’, XJ Yao’, . SYNTHESIS OF N-(4-CARBOMETHOXY-4-PHTHALIMIDOBUTANOYL)-N-SUBSTITUTED GLYCINES，PROLINE AND PYROGLUTAMIC ACIDJ. Acta Pharmaceutica Sinica, 1994, 29(5): 346-354.
Citation: WQ Lin, CY Cai, KS Gong, Y Wu, Z Long, XX Luo’, L Yang’, JF Li’, XJ Yao’, . SYNTHESIS OF N-(4-CARBOMETHOXY-4-PHTHALIMIDOBUTANOYL)-N-SUBSTITUTED GLYCINES，PROLINE AND PYROGLUTAMIC ACIDJ. Acta Pharmaceutica Sinica, 1994, 29(5): 346-354.
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N-(4-甲氧羰基-4-邻苯二甲酰亚氨基丁酰基)-N-取代甘氨酸、脯氨酸和焦谷氨酸的合成

SYNTHESIS OF N-(4-CARBOMETHOXY-4-PHTHALIMIDOBUTANOYL)-N-SUBSTITUTED GLYCINES，PROLINE AND PYROGLUTAMIC ACID

    摘要
  • 摘要: 报道11个预期有血管紧张素转化酶抑制活性的N-(4-甲氧羰基-4-邻苯二甲酰亚氨基丁酰基)-N-取代甘氨酸(VII1～9)、脯氨酸(VII10)和焦谷氨酸(VIl11)的合成和鉴定。所有上述化合物以及与VⅡ1～9相应的叔丁酯(VI1～9)均未见文献报道。药理初试结果显示，化合物VII8，VII9和VI10均有明显降压活性。

     

    Abstract: This paper reports the synthesis of eleven N-(4-carbomethoxy-4-phthalimidobu-tanoyl)-N-substituted glycines(VⅡ1～9)，proline(VⅡ10)and pyroglutamic acid(VⅡ11)expected tohave inhiMtory activity on angiotensin converting enzyme．All of the compounds mentioned above and the corresponding t-butyl esters of VⅡ1～9 were not reported in the literature previously．The structures were confirmed through their IR，1HNMR，MS spectra and elemental analysis．In preliminary test in rats,compounds VII8，VII9 and VII10 showed marked hypotensive activity．

     

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