title: Synthesis and structure-activity relationships of 7 beta-[(Z)-2-(2- aminothiazol-4-yl)-3-(substituted)-2-propenoyl-amino]-3- desacetoxymethylcephalosporins.
abstract: Synthesis and biological activity of a series of 7 beta-[(Z)-2-(2- aminothiazol-4-yl)-3-(substituted)-2-propenoylamino]-3-cephe m-4-carboxylic acids and their pivaloyloxymethyl esters are described. These acid compounds exhibited potent antibacterial activity against both Gram-positive and Gram-negative bacteria. Pivaloyloxymethyl esters of selected compounds in this series were found to be well absorbed from small intestine in mice.
authors.affiliation: Shionogi Research Laboratories, Shionogi & Co., Ltd., Osaka, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Ishikura
authors.forename: T
authors.initials: T
authors.lastname: Kubota
authors.forename: K
authors.initials: K
authors.lastname: Minami
authors.forename: Y
authors.initials: Y
authors.lastname: Hamashima
authors.forename: H
authors.initials: H
authors.lastname: Nakashimizu
authors.forename: K
authors.initials: K
authors.lastname: Motokawa
authors.forename: T
authors.initials: T
authors.lastname: Yoshida
mesh_terms: D000818:Animals; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D007408:Intestinal Absorption; D007421:Intestine, Small / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
chemical_list: D002511:Cephalosporins