Novel pyrazole derivatives as potent inhibitors of type II topoisomerases.: Part 1:: Synthesis and preliminary SAR analysis

被引：92

作者：

Gomez, Laurent ^{[1
]}

Hack, Michael D. ^{[1
]}

Wu, Jiejun ^{[1
]}

Wiener, John J. M. ^{[1
]}

Venkatesan, Hari ^{[1
]}

Santillan, Alejandro, Jr. ^{[1
]}

Pippel, Daniel J. ^{[1
]}

Mani, Neelakandha ^{[1
]}

Morrow, Brian J. ^{[1
]}

Motley, S. Timothy ^{[1
]}

Shaw, Karen Joy ^{[1
]}

Wolin, Ronald ^{[1
]}

Grice, Cheryl A. ^{[1
]}

Jones, Todd K. ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev LLC, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 10期

关键词：

gyrase; topoisomerase; pyrazoles; SAR; tetrahydroindazole;

D O I：

10.1016/j.bmcl.2007.03.003

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In an attempt to search for a new class of antibacterial agents, we have discovered a series of pyrazole analogs that possess good antibacterial activity for Gram-positive and Gram-negative organisms via inhibition of type II bacterial topoisomerases. We have investigated the structure-activity relationships of this series, with an emphasis on the length and conformation of the linker. This work led to the identification of tetrahydroindazole analogs, such as compound 1, as the most potent class of compounds. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：2723 / 2727

页数：5

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