Next Article in Journal
Regioselective Synthesis, Characterization, and Antimicrobial Activities of Some New Monosaccharide Derivatives
Previous Article in Journal
Synthesis and Biological Activities of Camphor Hydrazone and Imine Derivatives
Article Menu

Export Article

Open AccessArticle
Sci. Pharm. 2016, 84(3), 484-496; doi:10.3390/scipharm84030484

Benzotriazole-Mediated Synthesis and Antibacterial Activity of Novel N-Acylcephalexins

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Tabuk, Tabuk 71491, Saudi Arabia
Department of Microbiology and Immunology, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt
Author to whom correspondence should be addressed.
Academic Editor: Thomas Erker
Received: 13 December 2015 / Accepted: 18 February 2016 / Published: 13 April 2016
View Full-Text   |   Download PDF [6080 KB, uploaded 19 September 2016]   |  


Cephalexin (1) was acylated using N-acylbenzotriazoles (3ak′) derived from various carboxylic acids including aromatic, heterocyclic and N-Pg-α-amino acid to afford N-acylcephalexins in excellent yields (82%–96%). Antibacterial screening of the novel cephalosporins revealed that all targets (4aj) retained the antibacterial activity of cephalexin against Staphylococcus aureus (ATCC 6538). N-Nicotinylcephalexin (4c) and N-(3,4,5-trimethoxybenzoyl)cephalexin (4g) exhibited a broader spectrum of antibacterial activity towards standard strains of Staphylococcus aureus (ATCC 6538), Paenibacillus polymyxa (ATCC 842), and Escherichia coli (ATCC 10536) as well as a resistant strain of Pseudomonas aeruginosa (ATCC 27853). View Full-Text
Keywords: acylation; antibiotics; benzotriazolides; drug research acylation; antibiotics; benzotriazolides; drug research

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Supplementary material

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Agha, K.A.; Abo-Dya, N.E.; Ibrahim, T.S.; Abdel-Aal, E.H.; Hegazy, W.A. Benzotriazole-Mediated Synthesis and Antibacterial Activity of Novel N-Acylcephalexins. Sci. Pharm. 2016, 84, 484-496.

Show more citation formats Show less citations formats

Article Metrics

Article Access Statistics



[Return to top]
Sci. Pharm. EISSN 2218-0532 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top