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[Structure-activity relationship of oral cephalosporins]. 1989

E Bingen, and N Lambert-Zechovsky
Laboratoire de Microbiologie, Hôpital Robert Debré, Paris.

The advances achieved in the field of oral cephalosporins consist of improved bioavailability and enhanced intrinsic activity of the compounds. Oral absorption is facilitated either by creating prodrugs or by modifying the compound itself with addition of the alpha-amino group at position 7 on the cephem ring or of a vinyl group at position 3. Antibacterial activity and resistance to beta-lactamases are facilitated by the presence of an amino-2-thiazole heterocycle at position 7, associated with a methoxy-imino group or an oxy-imino-acetoxy group.

UI MeSH Term Description Entries
D002439 Cefotaxime Semisynthetic broad-spectrum cephalosporin. Benaxima,Biosint,Cefotaxim,Cefotaxime Sodium,Cefradil,Cephotaxim,Claforan,Fotexina,HR-756,Kendrick,Klaforan,Primafen,Ru-24756,Taporin,HR 756,HR756,Ru 24756,Ru24756,Sodium, Cefotaxime
D002444 Cefuroxime Broad-spectrum cephalosporin antibiotic resistant to beta-lactamase. It has been proposed for infections with gram-negative and gram-positive organisms, GONORRHEA, and HAEMOPHILUS. Cephuroxime,Ketocef,Zinacef
D002511 Cephalosporins A group of broad-spectrum antibiotics first isolated from the Mediterranean fungus ACREMONIUM. They contain the beta-lactam moiety thia-azabicyclo-octenecarboxylic acid also called 7-aminocephalosporanic acid. Antibiotics, Cephalosporin,Cephalosporanic Acid,Cephalosporin,Cephalosporin Antibiotic,Cephalosporanic Acids,Acid, Cephalosporanic,Acids, Cephalosporanic,Antibiotic, Cephalosporin,Cephalosporin Antibiotics
D006090 Gram-Negative Bacteria Bacteria which lose crystal violet stain but are stained pink when treated by Gram's method. Gram Negative Bacteria
D006094 Gram-Positive Bacteria Bacteria which retain the crystal violet stain when treated by Gram's method. Gram Positive Bacteria
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000042 Absorption The physical or physiological processes by which substances, tissue, cells, etc. take up or take in other substances or energy.
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D020682 Cefixime A third-generation cephalosporin antibiotic that is stable to hydrolysis by beta-lactamases. Cefixime Anhydrous,Cefixime Trihydrate,FK 027,FK-027,FR-17027,Suprax,FK027,FR 17027,FR17027

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