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

被引：59

作者：

Hoemann, MZ ^{[1
]}

Kumaravel, G ^{[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 | 2000年 / 10卷 / 23期

关键词：

D O I：

10.1016/S0960-894X(00)00542-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel structural class of antibacterials, 2-(1H-indol-3-yl)quinolines, effective against methicillin-resistant Staphylococcus aureus (MRSA), was discovered from a combinatorial library. A structure-activity relationship (SAR) study was conducted to determine the pharmacophore and increase the potency of these compounds. Compounds were prepared that had minimum inhibitory concentrations (MICs) < 1.0 <mu>g/mL against MRSA and retained activity against two strains of glycopeptide intermediate-resistant S. aureus (GISA). (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2675 / 2678

页数：4

共 5 条

[1] CHU DTW, 1998, ANNU REP MED CHEM, V33, P141
[2] DOEBNER O, 1883, BER, V16, P2357
[3] Methicillin-resistant Staphylococcus aureus clinical strain with reduced vancomycin susceptibility
Hiramatsu, K
Hanaki, H
Ino, T
Yabuta, K
Oguri, T
Tenover, FC
[J]. JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 1997, 40 (01) : 135 - 136
[4] Solid-phase synthesis of substituted quinoline and isoquinoline derivatives using heterocyclic N-oxide chemistry
Hoemann, MZ
Melikian-Badalian, A
Kumaravel, G
Hauske, JR
[J]. TETRAHEDRON LETTERS, 1998, 39 (27) : 4749 - 4752
[5] HOLMES RE, 1975, Patent No. 3870712

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