title: Synthesis and antimicrobial activity of certain new 1,2,4-triazolo[1,5-a]pyrimidine derivatives.
abstract: Certain new derivatives of 1,2,4-triazolo[1,5-a]pyrimidines were synthesized through the reaction of 1,2,4-triazolo[1,5-a]pyrimidine-7-ol with ethyl bromoacetate to afford the ethyl acetate ester, which upon hydrazinolysis gives the corresponding hydrazide. The hydrazide is the key intermediate which was used for the synthesis of the target compounds. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their in vitro antibacterial and antifungal activities. Most of the tested compounds showed comparable results with those of ampicillin and fluconazole reference drugs.
authors.affiliation: Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut-71526, Egypt.
authors.forename: Yaser A-H
authors.initials: YA
authors.lastname: Mostafa
authors.forename: Mostafa A
authors.initials: MA
authors.lastname: Hussein
authors.forename: Awwad A
authors.initials: AA
authors.lastname: Radwan
authors.forename: Abd El-Hamid N
authors.initials: Ael-H
authors.lastname: Kfafy
mesh_terms: D000085:Acetates / Q000737:chemistry; D000667:Ampicillin / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D015725:Fluconazole / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects* / Q000254:growth & development; D006094:Gram-Positive Bacteria / Q000187:drug effects* / Q000254:growth & development; D006842:Hydrocarbons, Brominated / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008826:Microbial Sensitivity Tests; D003904:Mitosporic Fungi / Q000187:drug effects* / Q000254:growth & development; D015394:Molecular Structure; D011743:Pyrimidines / Q000138:chemical synthesis / Q000494:pharmacology*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: C494034:1,2,4-triazolo(1,5-c)pyrimidine; D000085:Acetates; D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D006842:Hydrocarbons, Brominated; D011743:Pyrimidines; D014230:Triazoles; D000667:Ampicillin; D015725:Fluconazole; C010144:ethyl bromoacetate