Year-end Sale % OFF 
Abstract
New derivatives of 7-aminocephalosporanic acid 1–8 were synthesized by acylation of the 7-amino group of the cephem nucleus with various arylidinimino-1,3,4-thiadiazole-thio(or dithio)-acetic acid intermediates 3a–d and 5a–d, respectively, so the acyl side chains of these new cephalosporins contained a sulfide or disulfide bond. This unique combination of a Schiff base with the sulfide or disulfide bonds in the acyl side chain afforded new cephalosporins of reasonable potencies, some of which were found to possess moderate activities against the tested microorganisms. Their chemical structures were characterized by ¹H-NMR, IR spectroscopy and elemental microanalysis. Preliminary in vitro antimicrobial activities of the prepared cephalosporins were investigated using a panel of selected microorganisms. Results indicated that the newly synthesized cephalosporins containing disulfide bonds (compounds 5–8) exhibited better activities against Staphylococcus aureus and Escherichia coli. The cephalosporins cross-linked by a sulfide bond (compounds 1–4) showed a slight change in antimicrobial activities when compared with that of the reference cephalosporin (cephalexin).
Highlights
Cephalosporin molecules containing heterocyclic moieties as part of the acyl side chain substituents at the C7 position have become increasingly popular in cephalosporin research [1,2,3,4]
A successful cephalosporin containing a 1,3,4-thiadiazole moiety at the C3 position of the cephem nucleus showed a good improvement in activity against Pseudomonas aeruginosa and members of the Enterobactericae with higher serum levels [5,6]
Spectral and analytical data of the newly synthesized cephalosporins were all in good agreement with the proposed chemical structures
Summary
Cephalosporin molecules containing heterocyclic moieties as part of the acyl side chain substituents at the C7 position have become increasingly popular in cephalosporin research [1,2,3,4]. Certain cephalosporins containing a 1,2,4-thiadiazole moiety linked at the C7 acyl side chain were very potent, with improved MICs values [7,8,9]. The presence of sulfur can have a great contributions to the antimicrobial activities [15,16]. Disulfide derivatives of 1,3,4-thiadiazole have shown antimicrobial activities against
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
