| 摘要 |
<p>PURPOSE:To provide the subject novel compound having high antibacterial activity against sensitive/resistant gram-positive and gram-negative bacteria and high stability to beta-lactamase and DHP-I, thus useful as an antibacterial agent. CONSTITUTION:The objective compound of formula I [R<1> is H or methyl; R<2> is H or negative charge; (m) is 0-4; A is NR<3>R<4> [R<3> and R<4> are each H, alkyl, alkenyl, (CH2)n-NR<5>R<6> (R<5> and R<6> are each H or alkyl; (n) is 1-3), etc.], of formula II [B is O, S, SO, SO2, NR<10> (R<10> is alky, H, alkenyl, alkanoyl, carbamoyl, etc.), etc.] or pharmaceutically permissible salt or ester thereof, e.g.(5R, 6S)-6-[(R)-1-hydroxyethyl]-2-[(2S,4S)-2-sulfamoylmethylpyrr9lidine-4-y lthio]-1- carbapen-2-em-3-carboxylic acid. This compound and ba obatined by reaction of a compound of formula II or its reactive derivative with a compound of formula III and then, if needed, removing the protecting group.</p> |
