title: Synthesis of 2-oxoquinoline-3-carboxamide of ampicillin and amoxicillin as inhibitors of penicillin binding protein 1A of pseudomonas aeruginosa.
abstract: A series of ampicillin and amoxicillin derivatives were prepared by N-acylation with N1-substituted 1, 2-dihydro-2-oxoquinoline carboxylic acids by Schotten-Baumann procedure and evaluated as inhibitors of Pseudomonas aeruginosa using molecular docking study. Most of the derivatives showed remarkableactivity against Gram positive and Gram negative bacteria in vitro.
authors.affiliation: Department of Chemistry, Department of Biophysics, University of Mumbai, Vidynagari, Kalina, Santacruz (East), Mumbai 400 098, India.
authors.forename: Jayant
authors.initials: J
authors.lastname: Shelke
authors.forename: Gangadhar
authors.initials: G
authors.lastname: Meshram
authors.forename: Prabhkar
authors.initials: P
authors.lastname: Dongre
mesh_terms: D000215:Acylation; D000658:Amoxicillin / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D000667:Ampicillin / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001665:Binding Sites; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D046915:Penicillin-Binding Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D011487:Protein Conformation; D011550:Pseudomonas aeruginosa / Q000187:drug effects* / Q000254:growth & development / Q000378:metabolism; D015363:Quinolones / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D046915:Penicillin-Binding Proteins; D015363:Quinolones; D000667:Ampicillin; D000658:Amoxicillin