Meerpoel Lieven, Van Gestel Jef, Van Gerven Frans, Woestenborghs Filip, Marichal Patrick, Sipido Vic, Terence Gilkerson, Nash Roger, Corens David, Richards Ray D
Johnson & Johnson Pharmaceutical Research & Development, A Division of Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium.
Bioorg Med Chem Lett. 2005 Jul 15;15(14):3453-8. doi: 10.1016/j.bmcl.2005.05.007.
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.
