Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid

Autor(en): Persch, Elke
Basile, Teodora
Bockelmann, Svenja 
Huss, Markus 
Wieczorek, Helmut 
Carlomagno, Teresa
Menche, Dirk 
Stichwörter: Antibiotics; Archazolid; BINDING; Chemistry; Chemistry, Medicinal; Chemistry, Organic; CYSTOBACTER-VIOLACEUS; Derivative; HIGHLY POTENT; MYXOBACTERIA; Pharmacology & Pharmacy; Structure-activity data; SUBUNIT-C; V-ATPase; VACUOLAR; Water-solubility
Erscheinungsdatum: 2012
Herausgeber: PERGAMON-ELSEVIER SCIENCE LTD
Enthalten in: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Band: 22
Ausgabe: 24
Startseite: 7735
Seitenende: 7738
Zusammenfassung: 
The water-solubility of the highly potent V-ATPase inhibitors archazolid A and the glucosylated derivative archazolid C was studied in the presence of a wide range of cosolvents, revealing very low solubilites. The first water-soluble analogue was then designed, synthesized, and evaluated for V-ATPase inhibitory activity in vitro. (C) 2012 Elsevier Ltd. All rights reserved.
ISSN: 0960894X
DOI: 10.1016/j.bmcl.2012.09.081

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