Potent in vitro methicillin-resistant Staphylococcus aureus activity of 2-(1H-indol-3-yl)tetrahydroquinoline derivatives

被引：45

作者：

Hoemann, MZ ^{[1
]}

Xie, RL ^{[1
]}

Rossi, RF ^{[1
]}

Meyer, S ^{[1
]}

Sidhu, A ^{[1
]}

Cuny, GD ^{[1
]}

Hauske, JR ^{[1
]}

机构：

[1] Sepracor Inc, Marlborough, MA 01752 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(01)00714-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel antibacterials agents, 2-(1H-indol-3-yl) tetrahydroquinolines, were prepared using hetero Diels-Alder chemistry and found to be effective in vitro against methicillin-resistant Staphylococcus aureus (MRSA). A structure-activity relationship (SAR) study was conducted to determine the important features of this series and to increase the potency of these compounds. Compounds were prepared that had minimum inhibitory concentrations (MIC's) < 1.0 mug/mL against MRSA, but had no activity versus vancomycin- resistant Enterococcus (VRE). (C) 2002 Elsevier Science Ltd.

引用

页码：129 / 132

页数：4

共 4 条

[1] Patent in vitro methicillin-resistant Staphylococcus aureus activity of 2-(1H-indol-3-yl)quinoline derivatives
Hoemann, MZ
Kumaravel, G
Xie, RL
Rossi, RF
Meyer, S
Sidhu, A
Cuny, GD
Hauske, JR
[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2000, 10 (23) : 2675 - 2678
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KOBAYASHI, S
ISHITANI, H
NAGAYAMA, S
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[3] KOBAYASHI S, 1995, SYNTHESIS-STUTTGART, P1195
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