STUDIES ON β-LACTAM ANTIBIOTICS: XII. SYNTHESIS AND ACTIVITY OF NEW 3-ETHYNYLCEPHALOSPORIN

The synthesis of the orally absorbed 3-ethynylcephalosporin (1b) is described. In addition, the structure-activity relationships and oral absorption in rats of 7β-[(Z)-2-(2-amino-4-thiazolyl)-2-carboxymethoxyiminoacetamido]cephalosporins (1) having various aliphatic hydrocarbon groups at the 3-posit...

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Veröffentlicht in:	Journal of antibiotics 1986, Vol.39(3), pp.394-403
Hauptverfasser:	KAWABATA, KOHJI, MASUGI, TAKASHI, TAKAYA, TAKAO
Format:	Artikel
Sprache:	eng
Schlagworte:	Absorption Administration, Oral Animals Cephalosporins - chemical synthesis Cephalosporins - metabolism Chemistry Exact sciences and technology Heterocyclic compounds Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms Organic chemistry Preparations and properties Rats Rats, Inbred Strains Staphylococcus aureus - drug effects Structure-Activity Relationship
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Zusammenfassung:	The synthesis of the orally absorbed 3-ethynylcephalosporin (1b) is described. In addition, the structure-activity relationships and oral absorption in rats of 7β-[(Z)-2-(2-amino-4-thiazolyl)-2-carboxymethoxyiminoacetamido]cephalosporins (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.
ISSN:	0021-8820 1881-1469
DOI:	10.7164/antibiotics.39.394