Synthesis and anti-MRSA Activity of Novel Cephalosporin Derivatives
Cephalosporin derivatives containing a unique combination of lipophilic C-7 sidechains and polar C-3 thiopyridinium groups were synthesized and found to exhibit potent anti-MRSA activity in vitro and in vivo. The optimum C-7 sidechains utilized were 2,5-dichlorophenylthioacetamido and 2,6-dichloropy...
Saved in:
Published in: | Tetrahedron Vol. 56; no. 31; pp. 5687 - 5698 |
---|---|
Main Authors: | , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , |
Format: | Journal Article |
Language: | English |
Published: |
Elsevier Ltd
28-07-2000
|
Subjects: | |
Online Access: | Get full text |
Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
Summary: | Cephalosporin derivatives containing a unique combination of lipophilic
C-7 sidechains and polar
C-3 thiopyridinium groups were synthesized and found to exhibit potent
anti-MRSA activity in vitro and in vivo. The optimum
C-7 sidechains utilized were 2,5-dichlorophenylthioacetamido and 2,6-dichloropyrid-4-ylthioacetamido. The
C-3 thiopyridinium rings were substituted at nitrogen with amino acid and pyruvic acid groups that were designed to confer aqueous solubility as required for IV formulation. This paper describes the characteristics of these novel cephalosporins and highlights synthetic methods developed to allow their practical, large-scale syntheses. |
---|---|
ISSN: | 0040-4020 1464-5416 |
DOI: | 10.1016/S0040-4020(00)00418-X |