Synthesis and activity of new macrolones: Conjugates between 6(7)-(2′-aminoethyl)-amino-1-cyclopropyl-3-carboxylic acid (2′-hydroxyethyl) amides and 4"-propenoyl-azithromycin

被引：15

作者：

Kapic, Samra ^{[1
]}

Fajdetic, Andrea ^{[1
]}

Kostrun, Sanja ^{[1
]}

Cikos, Ana ^{[1
]}

Paljetak, Hana Cipcic ^{[1
]}

Antolovic, Roberto ^{[1
]}

Holmes, David J. ^{[2
]}

Alihodzic, Sulejman ^{[1
]}

机构：

[1] GlaxoSmithKline Res Ctr Zagreb Ltd, Zagreb 10000, Croatia

[2] GlaxoSmithKline, Collegeville, PA 19426 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2011年 / 19卷 / 23期

关键词：

Antimicrobial activity; Macrolides; Macrolones; Quinolone; Structure-activity relationship; PEPTIDYL TRANSFERASE CENTER; CONFORMATIONAL-ANALYSIS; STRUCTURAL BASIS; HIGHLY POTENT; ANTIBIOTICS; AZITHROMYCIN; KETOLIDES; TELITHROMYCIN; DERIVATIVES; RESISTANT;

D O I：

10.1016/j.bmc.2011.07.011

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 set of novel macrolones containing the flexible C8 basic linker and quinolone 3-(2 '-hydroxyethyl)carboxamido group has been prepared and structurally characterized by NMR and IR spectroscopy, mass spectrometry and molecular modeling. The new compounds were evaluated in vitro against a panel of erythromycin-susceptible and erythromycin-resistant Gram-positive and Gram-negative bacterial strains. Compared to azithromycin, most of the compounds exhibited improved in vitro potency against the key respiratory pathogens. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：7270 / 7280

页数：11

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