Derrick L.J Clive , Haikang Yang , Richard Z Lewanczuk
{"title":"血管紧张素转换酶抑制剂A58365A不可外渗类似物的合成及体外活性研究","authors":"Derrick L.J Clive , Haikang Yang , Richard Z Lewanczuk","doi":"10.1016/S1387-1609(01)01263-4","DOIUrl":null,"url":null,"abstract":"<div><p>The 3-methyl-substituted analog (±)-<strong>3</strong> of the angiotensin converting enzyme inhibitor A58365A (<strong>1</strong>) was synthesized from lactone <strong>4</strong> and amino acid ester <strong>16</strong>, via key intermediates <strong>18</strong>, <strong>19</strong> and <strong>21a</strong>,<strong>b</strong>. Compound (±)-<strong>3</strong> was found to possess powerful ACE inhibitory activity (<em>IC</em><sub>50</sub> = ca 500 nM), as judged by in vitro tests against porcine kidney ACE, under conditions in which the commercial drug captopril has <em>IC</em><sub>50</sub> = 280 nM.</p></div>","PeriodicalId":100305,"journal":{"name":"Comptes Rendus de l'Académie des Sciences - Series IIC - Chemistry","volume":"4 6","pages":"Pages 505-512"},"PeriodicalIF":0.0000,"publicationDate":"2001-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S1387-1609(01)01263-4","citationCount":"3","resultStr":"{\"title\":\"Synthesis and in vitro activity of a non-epimerizable analog of the angiotensin-converting enzyme inhibitor A58365A\",\"authors\":\"Derrick L.J Clive , Haikang Yang , Richard Z Lewanczuk\",\"doi\":\"10.1016/S1387-1609(01)01263-4\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>The 3-methyl-substituted analog (±)-<strong>3</strong> of the angiotensin converting enzyme inhibitor A58365A (<strong>1</strong>) was synthesized from lactone <strong>4</strong> and amino acid ester <strong>16</strong>, via key intermediates <strong>18</strong>, <strong>19</strong> and <strong>21a</strong>,<strong>b</strong>. Compound (±)-<strong>3</strong> was found to possess powerful ACE inhibitory activity (<em>IC</em><sub>50</sub> = ca 500 nM), as judged by in vitro tests against porcine kidney ACE, under conditions in which the commercial drug captopril has <em>IC</em><sub>50</sub> = 280 nM.</p></div>\",\"PeriodicalId\":100305,\"journal\":{\"name\":\"Comptes Rendus de l'Académie des Sciences - Series IIC - Chemistry\",\"volume\":\"4 6\",\"pages\":\"Pages 505-512\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2001-06-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/S1387-1609(01)01263-4\",\"citationCount\":\"3\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Comptes Rendus de l'Académie des Sciences - Series IIC - Chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S1387160901012634\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Comptes Rendus de l'Académie des Sciences - Series IIC - Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1387160901012634","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis and in vitro activity of a non-epimerizable analog of the angiotensin-converting enzyme inhibitor A58365A
The 3-methyl-substituted analog (±)-3 of the angiotensin converting enzyme inhibitor A58365A (1) was synthesized from lactone 4 and amino acid ester 16, via key intermediates 18, 19 and 21a,b. Compound (±)-3 was found to possess powerful ACE inhibitory activity (IC50 = ca 500 nM), as judged by in vitro tests against porcine kidney ACE, under conditions in which the commercial drug captopril has IC50 = 280 nM.
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