Synthesis and antibacterial activity of 1beta-methyl-2-(5-substituted thiazolidinopyrrolidin-3-ylthio)carbapenems and related compounds.
The synthesis of a new series of 1beta-methylcarbapenems containing the substituted thiazolidinopyrrolidine moiety is described. Their in vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of substituent on the thiazolidine ring was investigated.A particular compound (18 c) having a 2-amide substituted thiazolidine moiety showed the most potent antibacterial activity.
Medicinal Chemistry Research Center, Korea Institute of Science and Technology, Seoul, Korea.
Chang-Hyun
CH
Oh
Han-Won
HW
Cho
In-Kyu
IK
Lee
Jai-Yang
JY
Gong
Joung-Hoon
JH
Choi
Jung-Hyuck
JH
Cho
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D015780:Carbapenems / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008826:Microbial Sensitivity Tests; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000494:pharmacology; D013056:Spectrophotometry, Ultraviolet
D000900:Anti-Bacterial Agents; D015780:Carbapenems; D007202:Indicators and Reagents; D011759:Pyrrolidines