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

Elke Persch; Teodora Basile; Svenja Bockelmann; Markus Huss; Helmut Wieczorek; Teresa Carlomagno; Dirk Menche

doi:10.1016/j.bmcl.2012.09.081

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

Elke Persch, Teodora Basile, Svenja Bockelmann, Markus Huss, Helmut Wieczorek, Teresa Carlomagno, Dirk Menche

Biosciences

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Pages (from-to)	7735-8
Number of pages	4
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	22
Issue number	24
DOIs	https://doi.org/10.1016/j.bmcl.2012.09.081
Publication status	Published - 15 Dec 2012

Bibliographical note

Keywords

Dose-Response Relationship, Drug
Drug Design
Macrolides/chemical synthesis
Molecular Structure
Solubility
Structure-Activity Relationship
Thiazoles/chemical synthesis
Vacuolar Proton-Translocating ATPases/antagonists & inhibitors
Water/chemistry

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10.1016/j.bmcl.2012.09.081

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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.",

keywords = "Dose-Response Relationship, Drug, Drug Design, Macrolides/chemical synthesis, Molecular Structure, Solubility, Structure-Activity Relationship, Thiazoles/chemical synthesis, Vacuolar Proton-Translocating ATPases/antagonists & inhibitors, Water/chemistry",

author = "Elke Persch and Teodora Basile and Svenja Bockelmann and Markus Huss and Helmut Wieczorek and Teresa Carlomagno and Dirk Menche",

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AU - Persch, Elke

AU - Basile, Teodora

AU - Bockelmann, Svenja

AU - Huss, Markus

AU - Wieczorek, Helmut

AU - Carlomagno, Teresa

AU - Menche, Dirk

PY - 2012/12/15

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AB - 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.

KW - Dose-Response Relationship, Drug

KW - Drug Design

KW - Macrolides/chemical synthesis

KW - Molecular Structure

KW - Solubility

KW - Structure-Activity Relationship

KW - Thiazoles/chemical synthesis

KW - Vacuolar Proton-Translocating ATPases/antagonists & inhibitors

KW - Water/chemistry

U2 - 10.1016/j.bmcl.2012.09.081

DO - 10.1016/j.bmcl.2012.09.081

M3 - Article

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SN - 0960-894X

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SP - 7735

EP - 7738

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 24

ER -

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

Abstract

Bibliographical note

Keywords

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