Synthesis and mechanism of action of novel thiocarbamate inhibitors of human leukocyte elastase.

Li-Pan ZS; Joshi HV; Digenis GA

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Synthesis and mechanism of action of novel thiocarbamate inhibitors of human leukocyte elastase.

机译：人白细胞弹性蛋白酶的新型硫代氨基甲酸酯抑制剂的合成及其作用机理。

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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 P3 and ornithine at the P4 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.

机译：合成了几种人类白细胞弹性蛋白酶的肽基硫代氨基甲酸酯抑制剂，分子量范围为700-800。合成了两个不同的序列，赖氨酸在P3位置，鸟氨酸在P4位置。大多数具有大分子量的抑制剂表现出高抑制能力，Ki值低至10（-8）M。固定在平均分子量为36,000的聚α-β-[N-（2-羟乙基）-D，L-天冬酰胺]（PHEA）聚合物上的化合物显示出比其游离形式更高的抑制能力。

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《Journal of enzyme inhibition》 |2000年第1期|共15页
作者
Li-Pan ZS; Joshi HV; Digenis GA;
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正文语种 eng
中图分类生物化学;
关键词
Leukocyte Elastase; Serine Proteinase Inhibitors; Thiocarbamates; Indicators and Reagents; 白细胞弹性蛋白酶; 丝氨酸蛋白酶抑制剂; 硫代氨基甲酸酯类;

机译：Leukocyte Elastase;Serine Proteinase Inhibitors;Thiocarbamates;Indicators and Reagents;白细胞弹性蛋白酶;丝氨酸蛋白酶抑制剂;硫代氨基甲酸酯类;

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1. Synthesis and mechanism of action of novel thiocarbamate inhibitors of human leukocyte elastase. [J] . Li-Pan ZS, Joshi HV, Digenis GA Journal of enzyme inhibition . 2000,第1期

机译：人白细胞弹性蛋白酶的新型硫代氨基甲酸酯抑制剂的合成及其作用机理。
2. Synthesis and mechanism of action of novel thiocarbamate inhibitors of human leukocyte elastase. [J] . Li-Pan ZS, Joshi HV, Digenis GA Journal of enzyme inhibition . 2000,第1期

机译：人白细胞弹性蛋白酶的新型硫代氨基甲酸酯抑制剂的合成及其作用机理。
3. Synthesis and in-vitro evaluation of novel low molecular weight thiocarbamates as inhibitors of human leukocyte elastase. [J] . Rodis NP, Digenis GA Journal of enzyme inhibition . 2001,第2期

机译：新型低分子量硫代氨基甲酸酯类化合物作为人白细胞弹性蛋白酶抑制剂的合成及体外评价。
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机译：I：-核苷酸前药的设计，合成和研究。 II：5-氟-6-[（（2-氨基咪唑-1-基）甲基]尿嘧啶（AIFU）的合成及其作为胸苷磷酸化酶抑制剂的作用机理的研究。 III：-设计和合成新型核苷酸类似物作为研究底物胸苷酸合酶催化反应机理的替代底物。
6. Isolation, properties, and complete amino acid sequence of human secretory leukocyte protease inhibitor, a potent inhibitor of leukocyte elastase. [O] . R C Thompson, K Ohlsson 2015

机译：人分泌型白细胞蛋白酶抑制剂（一种有效的白细胞弹性蛋白酶抑制剂）的分离，性质和完整氨基酸序列。
7. Isolation, properties, and complete amino acid sequence of human secretory leukocyte protease inhibitor, a potent inhibitor of leukocyte elastase. [O] . Thompson, R C, Ohlsson, K 1986

机译：人分泌型白细胞蛋白酶抑制剂（一种有效的白细胞弹性蛋白酶抑制剂）的分离，性质和完整氨基酸序列。

Synthesis and mechanism of action of novel thiocarbamate inhibitors of human leukocyte elastase.

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