Synthesis and antibacterial activities of new 1beta-methylcarbapenems having aminopyrimidinylthioether moiety.
The synthesis of new 1beta-methylcarbapenems 1a-d bearing aminopyrimidinylthioether moiety at C-5 position of pyrrolidine ring and their antibacterial activities are described. All the compounds exhibited potent antibacterial activity. Of these carbapenems, 1d showed the best combination of antibacterial activity and stability to dehydropeptidase-I (DHP-I).
Lee
K S
KS
Medicinal Chemistry Research Center, Korea Institute of Science and Technology, Seoul, South Korea.
Lim
J H
JH
Kang
Y K
YK
Yoo
K H
KH
Kim
D C
DC
Shin
K J
KJ
Kim
D J
DJ
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D015780:Carbapenems / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D004150:Dipeptidases / Q000378:metabolism; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D013440:Sulfides / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D015780:Carbapenems; D011743:Pyrimidines; D013440:Sulfides; D004150:Dipeptidases; C038937:dipeptidase