RCM衍生的鲍曼-伯克抑制剂类似物的合成与生物测定。
Synthesis and bio-assay of RCM-derived Bowman-Birk inhibitor analogues.
作者信息
Miles Steven M, Leatherbarrow Robin J, Marsden Stephen P, Coates William J
机构信息
Department of Chemistry, Imperial College London, South Kensington Campus, London, UKSW7 2AZ.
出版信息
Org Biomol Chem. 2004 Feb 7;2(3):281-3. doi: 10.1039/b312908j. Epub 2003 Dec 24.
DOI:10.1039/b312908j
PMID:14747852
Abstract
Bowman-Birk inhibitor analogues containing 2, 3 and 4-carbon analogues of the natural disulfide were synthesised via solid phase microwave-assisted RCM and found to have K(i) values against chymotrypsin in the low to sub-micromolar range, the best replacement for the disulfide arising from the linkage by RCM of two l-homoallylglycine residues.
摘要
通过固相微波辅助复分解反应合成了含有天然二硫键的2碳、3碳和4碳类似物的鲍曼-伯克抑制剂类似物，发现它们对胰凝乳蛋白酶的抑制常数（K(i)）值在低至亚微摩尔范围内，由两个L-高烯丙基甘氨酸残基通过复分解反应连接形成的二硫键替代物效果最佳。
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