Synthesis and antibacterial evaluation of novel 2-[N-Imidoylpyrrolidinyl] carbapenems.
The synthesis, antibacterial activity and DHP-susceptibility of a series of novel carbapenems, directly linked with heterocyclic moiety are described. Especially, the compounds linked pyrrolidine-carbapenem exhibited to have a good antibacterial activity against Staphylococcus aureus (MRSA) as well as Pseudomonas aeruginosa to maintain a good stability towards DHP-I.
Hattori
Kouji
K
Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co. Ltd, 1-6, Kashima 2-Chome, Yodogawa-Ku, Osaka, Japan. kouji_hattori@po.fujisawa.co.jp
Yamada
Akira
A
Kuroda
Satoru
S
Chiba
Toshiyuki
T
Murata
Masayoshi
M
Sakane
Kazuo
K
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D015780:Carbapenems / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D004150:Dipeptidases / Q000378:metabolism; D006801:Humans; D007668:Kidney / Q000187:drug effects / Q000201:enzymology; D051379:Mice; D008826:Microbial Sensitivity Tests; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship; D013552:Swine
D000900:Anti-Bacterial Agents; D015780:Carbapenems; D004150:Dipeptidases; C038937:dipeptidase