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).

journal_name

Eur J Med Chem

authors

Kumar R,Nair RR,Dhiman SS,Sharma J,Prakash O

doi

10.1016/j.ejmech.2008.06.004

subject

Has Abstract

pub_date

2009-05-01 00:00:00

pages

2260-4

issue

5

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(08)00302-4

journal_volume

44

pub_type

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