Structure–activity relationship of new anti-tuberculosis agents derived from oxazoline and oxazole benzyl esters

During the syntheses and studies of natural iron chelators (mycobactins), we serendipitously discovered that a simple, small molecule, oxazoline-containing intermediate 3 displayed surprising anti-tuberculosis activity (MIC of 7.7 μM, average). Herein we report elaboration of SAR around this hit as...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	European journal of medicinal chemistry 2010-05, Vol.45 (5), p.1703-1716
Hauptverfasser:	Moraski, Garrett C., Chang, Mayland, Villegas-Estrada, Adriel, Franzblau, Scott G., Möllmann, Ute, Miller, Marvin J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Antitubercular Agents - chemical synthesis Antitubercular Agents - chemistry Antitubercular Agents - pharmacology Aryl oxazole Aryl oxazoline Benzyl ester Biological and medical sciences Disease Models, Animal Drug Evaluation, Preclinical Esters - chemical synthesis Esters - chemistry Esters - pharmacology Medical sciences Mice Mice, Inbred BALB C Molecular Conformation Mycobacterium tuberculosis - drug effects Mycobactins Oxazoles - chemical synthesis Oxazoles - chemistry Oxazoles - pharmacology Pharmacology. Drug treatments Stereoisomerism Structure-Activity Relationship Structure–activity relationships Tuberculosis - drug therapy Tuberculosis agents
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Schreiben Sie den ersten Kommentar!