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

Faculty Pharmacy Year: 2016
Type of Publication: ZU Hosted Pages:
Authors:
Wael Mohamed Ali Ali Abdelhakiem
Journal: Scientia Pharmaceutica mdpi Volume:
Keywords : Benzotriazole-Mediated Synthesis , Antibacterial Activity , Novel N-Acylcephalexins    
Abstract:
Cephalexin (1) was acylated using N-acylbenzotriazoles (3a–k′) 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 (4a–j) 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).
    
     
 
       

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