title: Antifungal agents, II: Synthesis and antifungal activities of aryl-1H-pyrrol-2-yl-1H-imidazol-1-yl-methane derivatives with unsaturated chains.
abstract: The synthesis and antifungal activities of aryl-1H-pyrrol-2-yl-1H-imidazol-1-yl-methanes having allyl, crotyl, and acrylate chains linked to the N-pyrrole atom and substituted at phenyl ring by Cl, F, CH3, and NO2 groups are reported. In vitro tests against Candida albicans and Candida spp. showed 2,4-dichlorophenyl-1-allyl-1H-pyrrol-2-yl-1H-imidazol-1-yl-methane to be the most potent derivative with activities comparable to those of ketoconazole and slightly inferior to those of bifonazole and miconazole. Some structure-activity relationships are discussed.
authors.affiliation: Dipartimento di Studi Farmaceutici, Università La Sapienza, Roma, Italy.
authors.forename: S
authors.initials: S
authors.lastname: Massa
authors.forename: R
authors.initials: R
authors.lastname: Ragno
authors.forename: G C
authors.initials: GC
authors.lastname: Porretta
authors.forename: A
authors.initials: A
authors.lastname: Mai
authors.forename: A
authors.initials: A
authors.lastname: Retico
authors.forename: M
authors.initials: M
authors.lastname: Artico
authors.forename: N
authors.initials: N
authors.lastname: Simonetti
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002175:Candida / Q000187:drug effects; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D008697:Methane / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000935:Antifungal Agents; D007093:Imidazoles; D011758:Pyrroles; D008697:Methane