“…Interest has focused in more recent investigations on vinylcephalosporins having a second substituent (R 2 ), e.g ., the development candidates TOC-39 and E1077 (Figure ). In contrast, cephalosporins tri-substituted (R 3 ≠ H) at the vinyl moiety, although known, − have so far received less attention. 1 …”
The synthesis and structure-activity relationships of a new class of vinylcephalosporins substituted with a lactamyl residue are described. These compounds show excellent activity against enterococci and retain the broad spectrum activity of third-generation cephalosporins such as ceftriaxone.
“…Interest has focused in more recent investigations on vinylcephalosporins having a second substituent (R 2 ), e.g ., the development candidates TOC-39 and E1077 (Figure ). In contrast, cephalosporins tri-substituted (R 3 ≠ H) at the vinyl moiety, although known, − have so far received less attention. 1 …”
The synthesis and structure-activity relationships of a new class of vinylcephalosporins substituted with a lactamyl residue are described. These compounds show excellent activity against enterococci and retain the broad spectrum activity of third-generation cephalosporins such as ceftriaxone.
“…During our extensive studies on the antibacterial activity and oral absorption of 719-[(Z)-2-(2-amino-4-thiazolyl)-2-carboxymethoxyiminoacetamido]cephalosporins1, 2) having various substituents at the 3-position of the cephem nucleus, we observed that compounds with relatively small substituents such as hydrogen, chloro, vinyl, methoxy, and methylthio exhibited higher oral absorptivity in rats.…”
The synthesis of the orally absorbed 3-ethynylcephalosporin (1b) is described. In addition, the structure-activity relationships and oral absorption in rats of 7(3-(1) having various aliphatic hydrocarbon groups at the 3-position are discussed. Of these cephalosporins (1), 3-ethynylcephalosporin (1b) exhibited better activity against Staphylococcus aureus than the other cephalosporins (1a, 1c and 1d) and showed moderate oral absorption in rats.
Von 7‐Aminocephalosporansäure (7‐ACS) ausgehend werden die 3‐α‐Chlorvinylcephalosporine 6, 7, 8, 9, 10 und 11 synthetisiert. 6, 7, 8, 9 und 10 sind Zwischenstufen für die neue antibakterielle Verbindung 11. Das Produkt 6 erhält man aus Acetylcephalosporin 5 und Triphenylphosphin in CCl4.
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