title: Synthesis and antifungal activity of pradimicin derivatives. Modifications on the aglycone part.
abstract: Synthesis and antifungal activity of pradimicin analogs modified on the aglycone part is described. Upon modification studies at various sites of the aglycone part using pradimicin A (PRM A), C-11 position was found to be the sole site to be modified without loosing antifungal activity. Further modification studies at C-11 position were carried out with 11-OH derivative of pradimicin T1 (PRM T1) because of its easy availability. Among the compounds prepared, 11-demethoxy derivative of PRM A (12) and 11-O-ethyl (13) and 11-O-fluoroethyl (14) derivatives of PRM T1 showed promising antifungal activity comparable to that of PRM A.
authors.affiliation: Bristol-Myers Squibb Research Institute, Bristol-Myers Squibb K. K., Tokyo, Japan.
authors.forename: S
authors.initials: S
authors.lastname: Aburaki
authors.forename: S
authors.initials: S
authors.lastname: Okuyama
authors.forename: H
authors.initials: H
authors.lastname: Hoshi
authors.forename: H
authors.initials: H
authors.lastname: Kamachi
authors.forename: M
authors.initials: M
authors.lastname: Nishio
authors.forename: T
authors.initials: T
authors.lastname: Hasegawa
authors.forename: S
authors.initials: S
authors.lastname: Masuyoshi
authors.forename: S
authors.initials: S
authors.lastname: Iimura
authors.forename: M
authors.initials: M
authors.lastname: Konishi
authors.forename: T
authors.initials: T
authors.lastname: Oki
mesh_terms: D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis* / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002240:Carbohydrate Sequence; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D008969:Molecular Sequence Data; D015394:Molecular Structure
chemical_list: D000903:Antibiotics, Antineoplastic; D000935:Antifungal Agents