{"title":"新型人白细胞弹性酶硫氨基甲酸酯抑制剂的合成及作用机制研究。","authors":"Sky Li-Pan Z, Joshi, Digenis","doi":"10.1080/14756369909030341","DOIUrl":null,"url":null,"abstract":"Several peptidyl thiocarbamate inhibitors of human leukocyte elastase were synthesized in the molecular weight range of 700-800. Two different sequences with lysine at the P(3) and ornithine at the P(4) positions were synthesized. Most of the inhibitors with large molecular weights showed high inhibitory capacity with Ki values as low as 10(-8) M. Compounds immobilized on poly,alpha,beta-[N-(2-hydroxyethyl)-d,l-aspartamide] (PHEA) polymers with an average molecular weight of 36,000 showed higher inhibitory capacity than their free forms.","PeriodicalId":15776,"journal":{"name":"Journal of enzyme inhibition","volume":"14 1","pages":"63-77"},"PeriodicalIF":0.0000,"publicationDate":"1999-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"2","resultStr":"{\"title\":\"Synthesis and Mechanism of Action of Novel Thiocarbamate Inhibitors of Human Leukocyte Elastase.\",\"authors\":\"Sky Li-Pan Z, Joshi, Digenis\",\"doi\":\"10.1080/14756369909030341\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Several peptidyl thiocarbamate inhibitors of human leukocyte elastase were synthesized in the molecular weight range of 700-800. Two different sequences with lysine at the P(3) and ornithine at the P(4) positions were synthesized. Most of the inhibitors with large molecular weights showed high inhibitory capacity with Ki values as low as 10(-8) M. Compounds immobilized on poly,alpha,beta-[N-(2-hydroxyethyl)-d,l-aspartamide] (PHEA) polymers with an average molecular weight of 36,000 showed higher inhibitory capacity than their free forms.\",\"PeriodicalId\":15776,\"journal\":{\"name\":\"Journal of enzyme inhibition\",\"volume\":\"14 1\",\"pages\":\"63-77\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"1999-11-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"2\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of enzyme inhibition\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.1080/14756369909030341\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of enzyme inhibition","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1080/14756369909030341","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Synthesis and Mechanism of Action of Novel Thiocarbamate Inhibitors of Human Leukocyte Elastase.
Several peptidyl thiocarbamate inhibitors of human leukocyte elastase were synthesized in the molecular weight range of 700-800. Two different sequences with lysine at the P(3) and ornithine at the P(4) positions were synthesized. Most of the inhibitors with large molecular weights showed high inhibitory capacity with Ki values as low as 10(-8) M. Compounds immobilized on poly,alpha,beta-[N-(2-hydroxyethyl)-d,l-aspartamide] (PHEA) polymers with an average molecular weight of 36,000 showed higher inhibitory capacity than their free forms.
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