Synthesis and in-vitro activity of novel 1beta-methylcarbapenems having spiro[2,4]heptane moieties.
The synthesis of a new series of 1beta-methylcarbapenems having spiro[2,4]heptane moieties is described. Their in-vitro antibacterial activities against both gram-positive and gram-negative bacteria were tested and the effect of substituents on the pyrrolidine ring was investigated. Most compounds were shown to be more active than the compared meropenem and imipenem against Escherichia coli. One particular compound, IIIb, having hydroxy a moiety showed the most potent antibacterial activity.
Park
Hyeong Beom
HB
Department of Chemistry, Hanyang University, Seoul, Korea.
Jo
Nam Hyun
NH
Hong
Joon Hee
JH
Choi
Jung Hoon
JH
Chei
Jung Hoon
JH
Cho
Jung-Hyuck
JH
Yoo
Kyung Ho
KH
Oh
Chang-Hyun
CH
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015780:Carbapenems / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
C476323:1 beta-methylcarbapenem; D000900:Anti-Bacterial Agents; D015780:Carbapenems; D013141:Spiro Compounds