Synthesis and biological properties of new 1 beta-methylcarbapenems.
The synthesis and biological activity of the novel series of 1 beta-methylcarbapenems, 1 and 2 were described. Most compounds displayed high potent antibacterial activity. The best compound in this series, 2a (IH201; R2 = NH2) showed an excellent and a broad spectrum as well as high renal DHP-I stability. It also possessed good in vivo efficacy and high safety.
Shin
K J
KJ
Medicinal Chemistry Research Center, Korea Institute of Science and Technology, Seoul, Korea.
Yoo
K H
KH
Kim
D J
DJ
Park
S W
SW
Ko
B S
BS
Lee
S J
SJ
Huh
J D
JD
Park
S Y
SY
D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D019540:Area Under Curve; D015780:Carbapenems / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D007928:Lethal Dose 50; D051379:Mice; D008826:Microbial Sensitivity Tests
D000890:Anti-Infective Agents; D015780:Carbapenems