title: Synthesis and antibacterial evaluation of amino acid-antibiotic conjugates.
abstract: Amino acid conjugates of quinolone, metronidazole and sulfadiazine antibiotics were synthesized in good yields using benzotriazole methodology. All the conjugates were screened for their antibacterial activity using methods adapted from the Clinical and Laboratory Standards Institute. Antibiotic conjugates were tested for activity in four medically relevant organisms; Staphylococcus aureus (RN4220), Escherichia coli (DH5α), Pseudomonas aeruginosa (PAO1), and Bacillus subtilis (168). Several antibiotic conjugates show promising results against several of the strains screened.
authors.affiliation: Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, United States; Department of Organic Chemistry, College of Pharmacy, Misr University for Science and Technology, Al-Motamayez District, PO Box 77, Egypt.
authors.forename: Mohamed A
authors.initials: MA
authors.lastname: Ibrahim
authors.affiliation: Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, United States.
authors.forename: Siva S
authors.initials: SS
authors.lastname: Panda
authors.affiliation: Department of Microbiology and Cell Science, University of Florida, Gainesville, FL 32611-7200, United States.
authors.forename: Antoinette S
authors.initials: AS
authors.lastname: Birs
authors.affiliation: Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, United States.
authors.forename: Juan C
authors.initials: JC
authors.lastname: Serrano
authors.affiliation: Department of Microbiology and Cell Science, University of Florida, Gainesville, FL 32611-7200, United States.
authors.forename: Claudio F
authors.initials: CF
authors.lastname: Gonzalez
authors.affiliation: Chemistry Department, King Abdulaziz University, Jeddah 21589 Saudi Arabia.
authors.forename: Khalid A
authors.initials: KA
authors.lastname: Alamry
authors.affiliation: Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, FL 32611-7200, United States; Chemistry Department, King Abdulaziz University, Jeddah 21589 Saudi Arabia. Electronic address: katritzky@chem.ufl.edu.
authors.forename: Alan R
authors.initials: AR
authors.lastname: Katritzky
mesh_terms: D000596:Amino Acids / Q000737:chemistry*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001412:Bacillus subtilis / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004926:Escherichia coli / Q000187:drug effects; D008795:Metronidazole / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D015363:Quinolones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship; D013411:Sulfadiazine / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000596:Amino Acids; D000900:Anti-Bacterial Agents; D015363:Quinolones; D013411:Sulfadiazine; D008795:Metronidazole
keywords: Antibacterial; Antibiotics; Benzotriazole; Conjugates; Lipophilicity