The effect of remote chirality on the antibacterial activity of indolinyl, tetrahydroquinolyl and dihydrobenzoxazinyl oxazolidinones

被引：27

作者：

Ciske, FL ^{[1
]}

Barbachyn, MR ^{[1
]}

Genin, MJ ^{[1
]}

Grega, KC ^{[1
]}

Lee, CS ^{[1
]}

Dolak, LA ^{[1
]}

Seest, EP ^{[1
]}

Watt, W ^{[1
]}

Adams, WJ ^{[1
]}

Friis, JM ^{[1
]}

Ford, CW ^{[1
]}

Zurenko, GE ^{[1
]}

机构：

[1] Pfizer, Kalamazoo, MI 49001 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 23期

关键词：

D O I：

10.1016/j.bmcl.2003.07.029

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The oxazolidinones are promising agents for the treatment of infections caused by gram-positive bacteria, including multidrug-resistant strains. In ongoing studies we have discovered that a strategically placed chiral center of appropriate absolute configuration improves the antibacterial activity of indolinyl oxazolidinone analogues (gram-positive MIC's < 0.5 mug/mL for the most potent congeners). The design, synthesis, antibacterial activity and pharmacokinetic profile of a selected series of a-methylated indoline derivatives and a related set of tetrahydroquinolyl and dihydrobenzoxazinyl analogues are discussed. (C) 2003 Published by Elsevier Ltd.

引用

页码：4235 / 4239

页数：5

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