title: Utility of Pyrazolylchalcone Synthon to Synthesize Azolopyrimidines under Grindstone Technology.
abstract: A series of pyrazolyl-triazolo[1,5-a]pyrimidines, pyrazolyl-tetrazolo[1,5-a]pyrimidines, pyrazolyl-benzo[4,5]imidazo[1,2-a]pyrimidines and bis-azolopyrimidines were prepared by reaction of pyrazolyl-chalcones or its bis-pyrazolyl-chalcones with the appropriate heterocyclic amines as aminotriazole, aminotetrazole, 2-aminobenzimidazole and 4,6-dimethyl-1H-pyrazolo[3,4-b]pyridin-3-amine by grinding method. The newly synthesized compounds have been characterized on the basis of elemental analysis and spectral data (IR,1H- and13C-NMR, Mass). Moreover, the newly synthesized products were screened for their in vitro antibacterial activities and the results showed that compounds 5f and 11d exhibited excellent activities compared with penicillin G and streptomycin as reference drugs.
authors.affiliation: Chemistry Department, Faculty of Science, Ain Shams University.
authors.forename: Maher Abd El-Aziz
authors.initials: MA
authors.lastname: El-Hashash
authors.forename: Sobhi Mohamed
authors.initials: SM
authors.lastname: Gomha
authors.forename: Elham Ezz
authors.initials: EE
authors.lastname: El-Arab
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001391:Azo Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D047188:Chalcones / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D001391:Azo Compounds; D047188:Chalcones; D011743:Pyrimidines; C000613925:pyrazolylchalcone