Synthesis of new 1-[2-Azido-2-(2,4-dichlorophenyl)ethyl]-1H/-imidazoles and in vitro evaluation of their antifungal activity

Francis Chevreuil; Anne Landreau; Denis Seraphin; Gérald Larcher; Jean-Philippe Bouchara; Pascal Richomme

doi:10.1080/14756360802205133

Synthesis of new 1-[2-Azido-2-(2,4-dichlorophenyl)ethyl]-1H/-imidazoles and in vitro evaluation of their antifungal activity

J Enzyme Inhib Med Chem. 2008 Oct;23(5):617-22. doi: 10.1080/14756360802205133.

Authors

Francis Chevreuil¹, Anne Landreau, Denis Seraphin, Gérald Larcher, Jean-Philippe Bouchara, Pascal Richomme

Affiliation

¹ EA 921, Laboratoire SONAS, UFR des Sciences Pharmaceutiques et Ingenierie de la Sante, Angers, France.

PMID: 18821251
DOI: 10.1080/14756360802205133

Abstract

New 1-[2-azido-2-(2,4-dichlorophenyl)ethyl]-1H/-imidazole were synthesized by nucleophilic substitution of various tertiary alcohols with azide anion in presence of boron trifluoride-diethyl etherate. Their antifungal activity was evaluated against Candida albicans, Candida glabrata, Aspergillus fumigatus and an azole-resistant petite mutant of C. glabrata. Preliminary SAR results are discussed.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Alcohols
Antifungal Agents / chemical synthesis*
Antifungal Agents / pharmacology
Aspergillus fumigatus / drug effects
Azides
Candida albicans / drug effects
Candida glabrata / drug effects
Imidazoles / chemical synthesis
Imidazoles / pharmacology*
Structure-Activity Relationship

Substances

Alcohols
Antifungal Agents
Azides
Imidazoles