title: Expansion of Antibacterial Spectrum of Muraymycins toward Pseudomonas aeruginosa.
abstract: It is urgent to develop novel anti-Pseudomonas agents that should also be active against multidrug resistant P. aeruginosa. Expanding the antibacterial spectrum of muraymycins toward P. aeruginosa was investigated by the systematic structure-activity relationship study. It was revealed that two functional groups, a lipophilic side chain and a guanidino group, at the accessory moiety of muraymycins were important for the anti-Pseudomonas activity, and analogue 29 exhibited antibacterial activity against a range of P. aeruginosa strains with the minimum inhibitory concentration values of 4-8 μg/mL.
authors.affiliation: Shionogi Innovation Center for Drug Discovery, Shionogi & Co., LTD. , Kita-21, Nishi-11 Kita-ku, Sapporo 001-0021, Japan.
authors.forename: Yusuke
authors.initials: Y
authors.lastname: Takeoka
authors.affiliation: Faculty of Pharmaceutical Sciences, Hokkaido University , Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan.
authors.forename: Tetsuya
authors.initials: T
authors.lastname: Tanino
authors.affiliation: Shionogi Innovation Center for Drug Discovery, Shionogi & Co., LTD. , Kita-21, Nishi-11 Kita-ku, Sapporo 001-0021, Japan.
authors.forename: Mitsuaki
authors.initials: M
authors.lastname: Sekiguchi
authors.affiliation: Shionogi Innovation Center for Drug Discovery, Shionogi & Co., LTD. , Kita-21, Nishi-11 Kita-ku, Sapporo 001-0021, Japan.
authors.forename: Shuji
authors.initials: S
authors.lastname: Yonezawa
authors.affiliation: Shionogi Innovation Center for Drug Discovery, Shionogi & Co., LTD. , Kita-21, Nishi-11 Kita-ku, Sapporo 001-0021, Japan.
authors.forename: Masahiro
authors.initials: M
authors.lastname: Sakagami
authors.affiliation: Shionogi Innovation Center for Drug Discovery, Shionogi & Co., LTD. , Kita-21, Nishi-11 Kita-ku, Sapporo 001-0021, Japan.
authors.forename: Fumiyo
authors.initials: F
authors.lastname: Takahashi
authors.affiliation: Shionogi Innovation Center for Drug Discovery, Shionogi & Co., LTD. , Kita-21, Nishi-11 Kita-ku, Sapporo 001-0021, Japan.
authors.forename: Hiroko
authors.initials: H
authors.lastname: Togame
authors.affiliation: Shionogi Innovation Center for Drug Discovery, Shionogi & Co., LTD. , Kita-21, Nishi-11 Kita-ku, Sapporo 001-0021, Japan.
authors.forename: Yoshikazu
authors.initials: Y
authors.lastname: Tanaka
authors.affiliation: Shionogi Innovation Center for Drug Discovery, Shionogi & Co., LTD. , Kita-21, Nishi-11 Kita-ku, Sapporo 001-0021, Japan.
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Takemoto
authors.affiliation: Faculty of Pharmaceutical Sciences, Hokkaido University , Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan ; Center for Research and Education on Drug Discovery, Hokkaido University , Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan.
authors.forename: Satoshi
authors.initials: S
authors.lastname: Ichikawa
authors.affiliation: Faculty of Pharmaceutical Sciences, Hokkaido University , Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan.
authors.forename: Akira
authors.initials: A
authors.lastname: Matsuda
keywords: Antibiotics; MraY; anti-Pseudomonas; drug-resistance; muraymycin; peptidoglycan