Effect of C-2 substitution on the stability of non-traditional cephalosporins in mouse plasma

Matthew Zimmerman; Stacey L McDonald; Hsin-Pin Ho-Liang; Patrick Porubsky; Quyen Nguyen; Cameron W Pharr; Andrew J Perkowski; Robert Smith; Frank J Schoenen; Ben S Gold; David Zhang; Carl F Nathan; Véronique Dartois; Jeffrey Aubé

doi:10.1038/s41429-019-0167-y

Effect of C-2 substitution on the stability of non-traditional cephalosporins in mouse plasma

J Antibiot (Tokyo). 2019 Jun;72(6):469-475. doi: 10.1038/s41429-019-0167-y. Epub 2019 Mar 22.

Authors

Affiliations

¹ Public Health Research Institute, New Jersey Medical School, Rutgers, the State University of New Jersey, Newark, NJ, 07013, USA.
² Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, USA.
³ Specialized Chemistry Center, University of Kansas, Lawrence, KS, 66045, USA.
⁴ Department of Microbiology and Immunology, Weill Cornell Medicine, New York, NY, 10065, USA.
⁵ Public Health Research Institute, New Jersey Medical School, Rutgers, the State University of New Jersey, Newark, NJ, 07013, USA. veronique.dartois@rutgers.edu.
⁶ Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC, 27599, USA. jaube@unc.edu.
⁷ Specialized Chemistry Center, University of Kansas, Lawrence, KS, 66045, USA. jaube@unc.edu.

Abstract

A systematic study of the stability of a set of cephalosporins in mouse plasma reveals that cephalosporins lacking an acidic moiety at C-2 may be vulnerable to β-lactam cleavage in mouse plasma.

Publication types

Research Support, N.I.H., Extramural
Research Support, Non-U.S. Gov't

MeSH terms

Animals
Anti-Bacterial Agents / blood*
Anti-Bacterial Agents / chemistry*
Cephalosporins / blood*
Cephalosporins / chemistry*
Mice
Molecular Structure
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Cephalosporins

Abstract

Publication types

MeSH terms

Substances

Grants and funding