新型刚性脒基苯丙氨酸衍生物作为凝血酶抑制剂的设计、合成及生物活性
Design, synthesis and biological activity of novel rigid amidino-phenylalanine derivatives as inhibitors of thrombin.
作者信息
Mack H, Pfeiffer T, Hornberger W, Böhm H J, Höffken H W
机构信息
Main Laboratory, Pharmaceuticals Research, Ludwigshafen, Germany.
出版信息
J Enzyme Inhib. 1995;9(1):73-86. doi: 10.3109/14756369509040682.
PMID:8568568
Abstract
(3S)-(Naphthalene-2-sulfonylamino)-1-[2R-(4-amidinophenyl)-1- piperidinocarbonylethyl]-2-pyrrolidinone (1a) is a potent inhibitor of thrombin with an IC50 value by 112 times lower than that of NAPAP (racemate). The selectivity versus trypsin can be improved by incorporation of substituents on the naphthyl ring. The mode of binding of the compound was determined by X-ray crystallography.
摘要
（3S）-（萘-2-磺酰氨基）-1-[2R-（4-脒基苯基）-1-哌啶羰基乙基]-2-吡咯烷酮（1a）是一种有效的凝血酶抑制剂，其IC50值比NAPAP（外消旋体）低112倍。通过在萘环上引入取代基，可以提高对胰蛋白酶的选择性。该化合物的结合模式通过X射线晶体学确定。
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