| 摘要 |
<p>PURPOSE:To obtain a new derivative for antimicrobial agents consisting of a cephem derivative having a substituted pyridinium group, excellent in antimicrobial action, especially exhibiting antimicrobial activity on methicillin- resistant Staphylococcus aureus and having a strong broad antimicrobial spectrum. CONSTITUTION:A chlorometylcephem compound expressed by formula I (R<1> is H or a protecting group of amino group; R<2> is H or a protecting group of hydroxyimino group; R<5> is H or a protecting group of carboxyl group; Q is CH or N) is dissolved in a solvent such as acetone and NaI is added to the solution under ice cooling and the compound of formula I is made to react with NaI to afford iodide and the iodide is made to react with a pyridine derivative having a substituent group of formula II [R<3> is a group substituted at 3-position or 4-position on pyridine ring, e.g. carbamoylmethyl, ureide, (substituted)thiazole or (substituted)thiadiazole] to provide the objective cephem derivative expressed by formula III [R<4> is a (protected)carboxyl or carboxylate) and useful as an antimicrobial agent, etc., for methicillin-resistant Staphylococcus aureus (MRSA).</p> |
