Synthesis and biological evaluation of NH2-acyl oseltamivir analogues as potent neuraniinidase inhibitors

被引：13

作者：

Wang, Kuanglei ^{[1
]}

Yang, Fei ^{[1
]}

Wang, Lihui ^{[2
]}

Liu, Kemin ^{[1
]}

Sun, Lu ^{[3
]}

Lin, Bin ^{[1
]}

Hu, Yaping ^{[1
]}

Wang, Boyu ^{[1
]}

Cheng, Maosheng ^{[1
]}

Tian, Yongshou ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Minist Educ, Key Lab Struct Based Drug Design & Discovery, 103 Wenhua Rd, Shenyang 110016, Liaoning, Peoples R China

[2] Shenyang Pharmaceut Univ, Sch Life Sci & Biopharmaceut Sci, 103 Wenhua Rd, Shenyang 110016, Liaoning, Peoples R China

[3] Shenyang Pharmaceut Univ, Sch Pharm, 103 Wenhua Rd, Shenyang 110016, Liaoning, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2017年 / 141卷

关键词：

Influenza virus; Neuraminidase inhibitors; Oseltamivir analogues; 150; cavity; INFLUENZA NEURAMINIDASE INHIBITORS; STRUCTURE-BASED DESIGN; STRUCTURAL-ANALYSIS; ANTIINFLUENZA ACTIVITY; PHOSPHONATE CONGENERS; ZANAMIVIR ANALOGS; PHOSPHATE TAMIFLU; DRUG DESIGN; IN-VITRO; DERIVATIVES;

D O I：

10.1016/j.ejmech.2017.10.004

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Neuraminidase inhibitors can deter nascent viruses from infecting intact cells by preventing their release from host cells. Herein, a neuraminidase inhibitor lib absent of basic moieties was discovered in the process of searching for inhibitors targeting 150 cavity. It exhibited potent inhibitions against wild-type neuraminidases from group 1 (H5N1 and H1N1) and group 2 (H7N9) subtypes with IC50 values similar to those of oseltamivir carboxylate. Moreover, lib showed moderate inhibitions against mutant neuraminidases from H5N1-H274Y and H1N1-H274Y with IC50 values of 2075 nM and 1382 nM, which were inferior to those of oseltamivir carboxylate (6095 nM and 4071 nM). The results were not consistent with the recognized SARs that a basic moiety was an indispensable part of a potent inhibitor. (C) 2017 Published by Elsevier Masson SAS.

引用

页码：648 / 656

页数：9

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