Synthesis and antibacterial activity of new carbapenems containing isoxazole moiety

The synthesis and biological activity of a series of new 1beta-methylcarbapenems 1a-g containing 5'-isoxazolopyrrolidin-3'-ylthio derivatives as C-2 side chain are described. Most compounds exhibited potent and well-balanced antibacterial activity as well as high stability to DHP-I compara...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-01, Vol.10 (2), p.95-99
Hauptverfasser:	YONG KOO KANG, KYE JUNG SHIN, KYUNG HO YOO, KYUNG JAE SEO, CHANG YONG HONG, LEE, C.-S, SEUNG YONG PARK, DONG JIN KIM, SANG WOO PARK
Format:	Artikel
Sprache:	eng
Schlagworte:	Anti-Bacterial Agents - chemical synthesis Anti-Bacterial Agents - pharmacology Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Biological and medical sciences Carbapenems - chemical synthesis Carbapenems - pharmacology Dipeptidases - metabolism Gram-Negative Bacteria - drug effects Gram-Positive Bacteria - drug effects Isoxazoles - chemical synthesis Isoxazoles - pharmacology Medical sciences Microbial Sensitivity Tests Molecular Structure Pharmacology. Drug treatments Stereoisomerism
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Zusammenfassung:	The synthesis and biological activity of a series of new 1beta-methylcarbapenems 1a-g containing 5'-isoxazolopyrrolidin-3'-ylthio derivatives as C-2 side chain are described. Most compounds exhibited potent and well-balanced antibacterial activity as well as high stability to DHP-I comparable to that of meropenem. 1e and 1c showed the best combination of antibacterial activity and stability to DHP-I, respectively.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(99)00646-0