结核菌酮类似物的合成及其抗病毒活性

Synthesis and antiviral activity of phthiobuzone analogues.

作者信息

Yang Ya-Jun, Zhao Jing-Hua, Pan Xian-Dao, Zhang Pei-Cheng

机构信息

Key Laboratory of Bioactive Substances and Resources Utilization of Chinese Herbal Medicine (Ministry of Education), Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, People's Republic of China.

出版信息

Chem Pharm Bull (Tokyo). 2010 Feb;58(2):208-11. doi: 10.1248/cpb.58.208.

DOI:10.1248/cpb.58.208

PMID:20118580

Abstract

A series of phthiobuzone analogs, prepared from potassium phthalimide or phthalandione, have been evaluated for their antiviral activities. Among the candidates, compounds 5j and 5k, which contain the substituted 4-halogenated phenyl ring at N-4',4'' position, show more potent antiviral activity than phthiobuzone against herpes simplex virus 1 (IC(50)=8.56 and 2.85 microg/ml, respectively) and herpes simplex virus 2 (IC(50)=1.75 and 4.11 microg/ml, respectively). Compounds 9c and 9d with a propylene linker between the phthalimide and bisthiosemicarbazone moieties display similar antiviral potency against herpes simplex virus 1 (IC(50)=2.85 and 4.11 microg/ml, respectively).

摘要

一系列由邻苯二甲酰亚胺钾或邻苯二酮制备的保泰松类似物已被评估其抗病毒活性。在这些候选物中，在N-4'，4'' 位置含有取代的4-卤代苯环的化合物5j和5k，对单纯疱疹病毒1（IC(50)分别为8.56和2.85微克/毫升）和单纯疱疹病毒2（IC(50)分别为1.75和4.11微克/毫升）显示出比保泰松更强的抗病毒活性。在邻苯二甲酰亚胺和双硫代半卡巴腙部分之间带有丙烯连接基的化合物9c和9d对单纯疱疹病毒1显示出相似的抗病毒效力（IC(50)分别为2.85和4.11微克/毫升）。