Discovery of a new class of antiviral compounds: Camphor imine derivatives

被引:86
作者
Sokolova, Anastasiya S. [1 ,2 ]
Yarovaya, Olga I. [1 ,2 ]
Shernyukov, Andrey V. [1 ]
Gatilov, Yuriy V. [1 ,2 ]
Razumova, Yuliya V. [2 ]
Zarubaev, Vladimir V. [3 ]
Tretiak, Tatiana S. [3 ]
Pokrovsky, Andrey G. [2 ]
Kiselev, Oleg I. [3 ]
Salakhutdinov, Nariman F. [1 ,2 ]
机构
[1] Russian Acad Sci, Siberian Branch, NN Vorozhtsov Novosibirsk Inst Organ Chem, Novosibirsk 630090, Russia
[2] Novosibirsk State Univ, Novosibirsk 630090, Russia
[3] Influenza Res Ctr, Dept Chemotherapy, St Petersburg 197376, Russia
基金
俄罗斯基础研究基金会; 俄罗斯科学基金会;
关键词
Influenza; Camphor derivatives; Antiviral; Cage compounds; IN-VITRO; INFLUENZA; VIRUS; AGENTS; ANTIINFLUENZA; RESISTANCE; INHIBITORS; MEMBRANE; DESIGN;
D O I
10.1016/j.ejmech.2015.10.010
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A new class of compounds featuring a camphor moiety has been discovered that exhibits potent inhibitory activity against influenza A(H1N1)pdm09 and A(H5N1) viruses. The synthesized compounds were characterized by spectroscopic analysis; in addition the structures of compound 2 and 14 were elucidated by the X-ray diffraction technique. Structure activity relationship studies have been conducted to identify the 1,7,7-trimethylbicyclo[2.2.1]heptanes2-ylidene group as the key functional group responsible for the observed antiviral activity. The most potent antiviral compound is imine 2 with therapeutic index more than 500. (C) 2015 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:263 / 273
页数:11
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