Microwave assisted one-pot synthetic route to imidazo[1,2-a]pyrimidine derivatives of imidazo/triazole clubbed pyrazole and their pharmacological screening

Abstract

An efficient synthesis of imidazo[1,2-a]pyrimidine derivatives of pyrazole in excellent yield over a short reaction time based on a microwave-assisted, one-pot three-component condensation reaction of pyrazole aldehyde clubbed with imidazole 4 and triazole 5 nuclei, (substituted-phenyl/hetero-aryl)ethanones 6(a–g), and 2-amino benzimidazole 7 in the presence of the strong base KOH is described. All the compounds were screened for their preliminary in vitro antimicrobial, antituberculosis and antimalarial activities against a panel of pathogenic strains. The majority of the compounds exhibited excellent inhibitory action against S. typhi, S. pneumoniae, B. subtilis, and C. tetani. Some of the compounds showed good antifungal activity and moderate antituberculosis activity as compared to first line drugs. Two of the compounds 8b and 9b exhibited excellent antimalarial activity against P. falciparum strains.