title: Syntheses and antifungal activity of dl-griseofulvin and its congeners. II.
abstract: Griseofulvin derivatives, dl-6'-demethyl-6'-ethylgriseofulvin (dl-5) and dl-6'demethyl-6'phenylgriseofulvin (dl-6) were prepared by application of a synthetic method developed by us. Antifungal activity of these derivatives decreased in the order of dl-griseofulvin (dl-1) >> dl-6(inactive). The reaction of these derivatives with ethanethiol gave two types of compounds, 2'-(ethylthio)griseofulvin (15) and 4'-(ethylthio)isogriseofulvin (16). The relationship between the ratios of isolated yield of 15 and 16 and antifungal the activity of griseofulvin derivatives is discussed.
authors.affiliation: Faculty of Pharmaceutical Sciences, Okayama University, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Takeuchi
authors.forename: H
authors.initials: H
authors.lastname: Tomozane
authors.forename: K
authors.initials: K
authors.lastname: Misumi
authors.forename: K
authors.initials: K
authors.lastname: Yata
authors.forename: T
authors.initials: T
authors.lastname: Kawata
authors.forename: Y
authors.initials: Y
authors.lastname: Niino
authors.forename: M
authors.initials: M
authors.lastname: Yamato
authors.forename: T
authors.initials: T
authors.lastname: Harayama
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D006118:Griseofulvin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D014249:Trichophyton / Q000187:drug effects
chemical_list: D000935:Antifungal Agents; D006118:Griseofulvin