Syntheses of 1beta-methylcarbapenems bearing 5-methyl-4-hydroxypyrrolidinone.
A new series of 1beta-methylcarbapenems 1a-d bearing 5-methyl-4-mercaptopyrrolidinone rings has been prepared and evaluated for in vitro antibacterial activity and pharmacokinetic parameters. Most compounds showed excellent antibacterial activity and high stability to dehydropeptidase-1. We have synthesized optically active 5-methyl-4-hydroxypyrrolidinones from enantiomerically pure aziridine esters.
Pyun
Do Kyu
DK
Korea Research Institute of Chemical Technology, Yusung, Taejon.
Kim
Bong Jin
BJ
Jung
Hee Jung
HJ
Kim
Jae Hak
JH
Lee
Jin Soo
JS
Lee
Won Koo
WK
Lee
Cheol Hae
CH
D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D015780:Carbapenems / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008826:Microbial Sensitivity Tests; D011760:Pyrrolidinones / Q000737:chemistry*
C465554:5-methyl-4-hydroxypyrrolidinone; D000890:Anti-Infective Agents; D015780:Carbapenems; D011760:Pyrrolidinones