4.5 Article

Pyrrolo[1,2-a][1,4]benzodiazepine:: A novel class of non-azole anti-dermatophyte anti-fungal agents

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 15, Issue 14, Pages 3453-3458

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.05.007

Keywords

anti-fungal; anti-dermatophyte; 4H-pyrrolo[1,2-a][1,4]benzodiazepine

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Broad screening revealed compound la to be a novel anti-fungal agent with high specificity towards dermatophytes. The anti-fungal structure-activity relationship of this novel class of 5,6-dihydro-4H-pyrrolo[1,2-a][1,4]benzodiazepines is described together with its mode of action that appeared to be the inhibition of squalene epoxidase. Preliminary in vivo results of the most active compounds are also reported. (c) 2005 Elsevier Ltd. All rights reserved.

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