title: Synthesis and structure-activity relations in the class of 2-(pyridyl)penems.
abstract: The isosteric CH----N substitution in the class of 2-arylpenems results in improved antibacterial activity, with retention of the favorable characteristic of stability towards renal dehydropeptidase. High therapeutic efficacy was demonstrated in experimental mice septicemias with the 2-(3-pyridyl) derivative 2b and its orally absorbed acetoxymethyl ester prodrug 4n.
authors.affiliation: Farmitalia Carlo Erba SpA, R. & D., Infectious Diseases Dept., Milan, Italy.
authors.forename: A
authors.initials: A
authors.lastname: Bedeschi
authors.forename: G
authors.initials: G
authors.lastname: Visentin
authors.forename: E
authors.initials: E
authors.lastname: Perrone
authors.forename: F
authors.initials: F
authors.lastname: Giudici
authors.forename: F
authors.initials: F
authors.lastname: Zarini
authors.forename: G
authors.initials: G
authors.lastname: Franceschi
authors.forename: G
authors.initials: G
authors.lastname: Meinardi
authors.forename: P
authors.initials: P
authors.lastname: Castellani
authors.forename: D
authors.initials: D
authors.lastname: Jabes
authors.forename: R
authors.initials: R
authors.lastname: Rossi
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D001419:Bacteria / Q000187:drug effects*; D004927:Escherichia coli Infections / Q000188:drug therapy; D005260:Female; D051379:Mice; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D018805:Sepsis / Q000188:drug therapy*; D013203:Staphylococcal Infections / Q000188:drug therapy; D013290:Streptococcal Infections / Q000188:drug therapy; D013329:Structure-Activity Relationship; D001618:beta-Lactamases / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D000900:Anti-Bacterial Agents; D011725:Pyridines; D001618:beta-Lactamases