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

…, J Van Gestel, F Van Gerven, F Woestenborghs…

Index: Meerpoel, Lieven; Van Gestel, Jef; Van Gerven, Frans; Woestenborghs, Filip; Marichal, Patrick; Sipido, Vic; Terence, Gilkerson; Nash, Roger; Corens, David; Richards, Ray D. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 14 p. 3453 - 3458

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Citation Number: 21

Abstract

Broad screening revealed compound 1a 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.