Synthesis and antiviral activity of a new series of 4-isothiazolecarbonitriles

被引：8

作者：

Cutrí, CCC

Garozzo, A

Siracusa, MA

Sarvá, MC

Tempera, G

Geremia, E

Pinizzotto, MR

Guerrera, F

机构：

[1] Univ Catania, Dipartimento Sci Farmaceut, I-95125 Catania, Italy

[2] Univ Catania, Dipartimento Sci Microbiol & Ginecol, I-95124 Catania, Italy

[3] Univ Catania, Ist Biol Gen, I-95124 Catania, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1998年 / 6卷 / 12期

关键词：

D O I：

10.1016/S0968-0896(98)80007-2

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of 4-isothiazolecarbonitriles was synthesized and screened for in vitro antiviral activity. The effect of various substituents on the phenyl ring, as well as the substitution of the phenyl for other aromatic and heteroaromatic rings, was examined to establish the requirements for optimum activity. The most active member of the series, 3-methylthio-5-phenyl-4-isothiazolecarbonitrile, exhibited a high level of activity against enteroviruses polio 1 and ECHO 9. Preliminary studies on its mechanism of action indicated that this compound had an effect on an early event in the replication of poliovirus type 1. (C) 1998 Published by Elsevier Science Ltd. All rights reserved.

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页码：2271 / 2280

页数：10

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