title: Pyrrolo[1,2-a][1,4]benzodiazepine: a novel class of non-azole anti-dermatophyte anti-fungal agents.
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.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development, A Division of Janssen Pharmaceutica N.V., Turnhoutseweg 30, B-2340 Beerse, Belgium. lmeerpoe@prdbe.jnj.com
authors.forename: Lieven
authors.initials: L
authors.lastname: Meerpoel
authors.forename: Jef
authors.initials: J
authors.lastname: Van Gestel
authors.forename: Frans
authors.initials: F
authors.lastname: Van Gerven
authors.forename: Filip
authors.initials: F
authors.lastname: Woestenborghs
authors.forename: Patrick
authors.initials: P
authors.lastname: Marichal
authors.forename: Vic
authors.initials: V
authors.lastname: Sipido
authors.forename: Gilkerson
authors.initials: G
authors.lastname: Terence
authors.forename: Roger
authors.initials: R
authors.lastname: Nash
authors.forename: David
authors.initials: D
authors.lastname: Corens
authors.forename: Ray D
authors.initials: RD
authors.lastname: Richards
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis / Q000145:classification* / Q000494:pharmacology*; D003883:Arthrodermataceae / Q000187:drug effects*; D001381:Azepines / Q000138:chemical synthesis / Q000145:classification / Q000494:pharmacology*; D015195:Drug Design; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011758:Pyrroles / Q000138:chemical synthesis / Q000145:classification / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D001381:Azepines; D011758:Pyrroles; C506245:Pyrrolo(1,2-a)(1,4)benzodiazepine