The synthesis of novel 1 beta-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.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/s0960-894x(02)00948-4 | DOI Listing |
Publication Analysis
Top Keywords
biological evaluation
8
novel beta-methylcarbapenems
8
synthesis biological
4
evaluation novel
4
beta-methylcarbapenems isothiazoloethenyl
4
isothiazoloethenyl side
4
side chains
4
chains synthesis
4
synthesis novel
4
beta-methylcarbapenems 1ab
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!