摘要 |
<p>PROBLEM TO BE SOLVED: To obtain the subject new derivatives comprising specific vinylpyrrolidinone cephalosporin derivatives and useful for treatment and prevention, etc., of diseases due to gram-positive bacteria, especially sensitive and resistant staphylococcus, Pneumococcus and enteric coccus. SOLUTION: The new vinylpyrrolidinone cephalosporin derivatives are represented by formula I [R<1> is a halogen, a (substituted)lower alkyl, a (substituted)phenyl, a (substituted)benzyl, a (substituted)heterocyclic group, etc.; R<2> is H, OH, a lower alkyl-Qr (Q is an alkylene, CO or SO2 ; (r) is 0 or 1), an aryl-Qr, etc.; R<3> is OH, a lower alkoxy, OM (M is an alkali metal), etc.; R<4> and R<5> are each H, a lower alkyl or phenyl; X is S, O, NH or CH2 ; (n) is 0, 1 or 2; (m) and (s) are each 0 or 1] and useful as a medicine, etc., for treatment and prevention of infectious diseases. The compound is obtained by treating a compound having formula II (R<f> is H or trimethylsilyl; R<g> is H, benzhydryl, etc.) with a carboxylic acid of formula III (Y is OH or its reactive derivative).</p> |