Pyrrolo[1,2-a][1,4]benzodiazepine: a novel class of non-azole anti-dermatophyte anti-fungal agents |
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| Authors: | Meerpoel Lieven Van Gestel Jef Van Gerven Frans Woestenborghs Filip Marichal Patrick Sipido Vic Terence Gilkerson Nash Roger Corens David Richards Ray D |
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| Affiliation: | Johnson & Johnson Pharmaceutical Research & Development, A Division of Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium. lmeerpoe@prdbe.jnj.com |
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| 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. |
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