Author/Authors :
Yong Koo Kang، نويسنده , , Kyung Seok Lee، نويسنده , , Kyung Ho Yoo، نويسنده , , Kye Jung Shin، نويسنده , , Dong Chan Kim، نويسنده , , Chang-Seok Lee، نويسنده , , Jae Yang Kong، نويسنده , , Dong Jin Kim، نويسنده ,
Abstract :
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.