title: 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.
abstract: 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.
authors: GlaxoSmithKline Research Centre Zagreb Ltd, Prilaz baruna Filipovića 29, 10000 Zagreb, Croatia. samra.kapic@glpg.com
authors: Samra
authors: S
authors: Kapić
authors: Andrea
authors: A
authors: Fajdetić
authors: Sanja
authors: S
authors: Koštrun
authors: Ana
authors: A
authors: Cikoš
authors: Hana Čipčić
authors: HČ
authors: Paljetak
authors: Roberto
authors: R
authors: Antolović
authors: David J
authors: DJ
authors: Holmes
authors: Sulejman
authors: S
authors: Alihodžić
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry; D017963:Azithromycin / Q000031:analogs & derivatives* / Q000138:chemical synthesis; D006801:Humans; D018942:Macrolides / Q000138:chemical synthesis* / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D018942:Macrolides; D015363:Quinolones; D017963:Azithromycin