title: Benzotriazole-Mediated Synthesis and Antibacterial Activity of Novel N-Acylcephalexins.
abstract: Cephalexin (1) was acylated usingN-acylbenzotriazoles (3a-k') derived from various carboxylic acids including aromatic, heterocyclic andN-Pg-α-amino acid to affordN-acylcephalexins in excellent yields (82%-96%). Antibacterial screening of the novel cephalosporins revealed that all targets (4a-j) retained the antibacterial activity of cephalexin againstStaphylococcus aureus(ATCC 6538).N-Nicotinylcephalexin (4c) andN-(3,4,5-trimethoxybenzoyl)cephalexin (4g) exhibited a broader spectrum of antibacterial activity towards standard strains ofStaphylococcus aureus(ATCC 6538),Paenibacillus polymyxa(ATCC 842), andEscherichia coli(ATCC 10536) as well as a resistant strain ofPseudomonas aeruginosa(ATCC 27853).
authors.affiliation: Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt. aghanet2010@yahoo.com.
authors.forename: Khalid A
authors.initials: KA
authors.lastname: Agha
authors.affiliation: Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt. nader_elmaghry88@yahoo.com.|Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Tabuk, Tabuk 71491, Saudi Arabia. nader_elmaghry88@yahoo.com.
authors.forename: Nader E
authors.initials: NE
authors.lastname: Abo-Dya
authors.affiliation: Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt. Tarekeldeeb1976@yahoo.com.
authors.forename: Tarek S
authors.initials: TS
authors.lastname: Ibrahim
authors.affiliation: Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt. eatedalabdelaal@yahoo.com.
authors.forename: Eatedal H
authors.initials: EH
authors.lastname: Abdel-Aal
authors.affiliation: Department of Microbiology and Immunology, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt. Wmhegazy@yahoo.com.
authors.forename: Wael A
authors.initials: WA
authors.lastname: Hegazy
keywords: acylation; antibiotics; benzotriazolides; drug research