title: Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid.
abstract: 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.
authors.affiliation: Institut für Organische Chemie, Ruprecht-Karls-Universität Heidelberg, INF 270, 69120 Heidelberg, Germany.
authors.forename: Elke
authors.initials: E
authors.lastname: Persch
authors.forename: Teodora
authors.initials: T
authors.lastname: Basile
authors.forename: Svenja
authors.initials: S
authors.lastname: Bockelmann
authors.forename: Markus
authors.initials: M
authors.lastname: Huss
authors.forename: Helmut
authors.initials: H
authors.lastname: Wieczorek
authors.forename: Teresa
authors.initials: T
authors.lastname: Carlomagno
authors.forename: Dirk
authors.initials: D
authors.lastname: Menche
mesh_terms: D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D018942:Macrolides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D012995:Solubility; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D025262:Vacuolar Proton-Translocating ATPases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D014867:Water / Q000737:chemistry
chemical_list: D018942:Macrolides; D013844:Thiazoles; C519727:archazolid A; D014867:Water; D025262:Vacuolar Proton-Translocating ATPases