title: Organoiodine (III)-mediated synthesis of 3-aryl/heteroaryl-5,7-dimethyl-1,2,4-triazolo[4,3-c]pyrimidines as antibacterial agents.
abstract: Synthesis of 12 new 3-aryl/heteroaryl-5,7-dimethyl-1,2,4-triazolo[4,3-c]pyrimidines (3a-l) has been accomplished by the oxidation of pyrimidinylhydrazones (2a-l) of various aryl/heteroaryl aldehydes using 1.1equiv. of iodobenzene diacetate (IBD) in dichloromethane. All the compounds 3a-l tested in vitro for their antibacterial activity against two Gram-positive bacteria namely, Bacillus subtilis, Bacillus stearothermophilus and two Gram-negative bacteria Pseudomonas putida, Escherichia coli. Two compounds, namely 3-(2,4-dichlorophenyl)-5,7-dimethyl-1,2,4-triazolo [4,3-c]pyrimidine (3j) and 3-(4-hydroxy-2-methoxyphenyl)-5,7-dimethyl-1,2,4-triazolo[4,3-c]pyrimidine (3l) were found to be equipotent or more potent than the commercially available antibiotics (chloramphenicol and streptomycin).
authors.affiliation: Department of Chemistry, Kurukshetra University, Kurukshetra 136119, India.
authors.forename: Ravi
authors.initials: R
authors.lastname: Kumar
authors.forename: Reshmi R
authors.initials: RR
authors.lastname: Nair
authors.forename: Saurabh Sudha
authors.initials: SS
authors.lastname: Dhiman
authors.forename: Jitender
authors.initials: J
authors.lastname: Sharma
authors.forename: Om
authors.initials: O
authors.lastname: Prakash
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D007455:Iodine; D011743:Pyrimidines / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D011743:Pyrimidines; D007455:Iodine