Bioorganic and Medicinal Chemistry Letters p. 463 - 466 (2003)
Update date:2022-08-03
Topics:
Kang, Yong Koo
Lee, Kyung Seok
Yoo, Kyung Ho
Shin, Kye Jung
Kim, Dong Chan
Lee, Chang-Seok
Kong, Jae Yang
Kim, Dong Jin
The synthesis of novel 1β-methylcarbapenems 1a,b bearing isothiazoloethenyl moieties at C-5 position of pyrrolidine ring and their biological evaluation are described. Both compounds showed potent and well-balanced antibacterial activity as well as high stability to DHP-I. Especially, 5-isothiazole derivative 1a exhibited excellent DHP-I stability and advanced pharmacokinetics profiles, compared to 5-isoxazole derivative 2, imipenem, and meropenem.
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