The cephalosporin antibiotics has been the mainstay of antibacterial chemotherapy for decades. Even though some of them have potent and well balanced antimicrobial activity, they are limitted to use for their poor oral absorption as expected from their physicochemical properties. In this case, introduction of pivaloyloxymethyl moiety to carboxylic acid of the cephalosporin nucleus is one of the approaches for improvement of oral absorption (e.g. cefcapene pivoxil). However, there is little improvement of some commercially available cepharosporins as injectable formulation using this approaches. Therefore we conducted exploratory research of new prodrugs including introduction of some carbamoyl group to aminothiazole of C-7 side chain of the cephalosporin nucleus. The details of synthesis, physicochemical properties, and PK profiles of some cephalosporin derivatives will be presented.

Exploratory research of novel prodrugs for enhancement of oral absorption of cephalosporin antibiotics

Macromolecular Chemistry: The Second Century

[Author Benefits](https://scimeetings.acs.org/?utm_source=pubs_content_marketing&utm_medium=website&utm_campaign=0320_MCF_NPI_Launch_Spring_Homepage&ref=pubs_content_marketing)

[How to use SciMeetings](https://storage.googleapis.com/dl.morressier.com/acs/SciMeetings-ACSSpring2020-HowToGuide_M3020-Final.pdf)

[Frequently Asked Questions](https://storage.googleapis.com/dl.morressier.com/acs/SciMtng_ACSNMSp2020_FAQ_M3120_Final.pdf)

ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.