Resumo:
Diseases caused by bacteria have been a major problem worldwide since they are
responsible for many deaths every year around the world and high health-related
costs. In addition, the drug resistance has been raised significantly. Therefore, it is very
relevant the research in order to developing new classes of antibacterial. There are
many reports in the literature showing that heterocyclic compounds containing nitrogen
atom have great biological potential, specially pyrazole moiety, which has showed
remarkable antimicrobial activity. Thus, in this work aimed to synthesize new seven
pyrazole derivatives 7-aryl-2,3,6,7-tetrahydro-5H-imidazo[1,2-c]pyrazolo[4,3-
e]pyrimidine-5-thiones 1(a-g). The raw materials 5-amino-1-aryl-1H-pyrazole-4-
carbonitriles 3(a-g) and the key intermediates 5-amino-1-aryl-4-(4,5-dihydro-1H imidazole-2-yl)-1H-pyrazoles 2(a-g) were obtained in 47 to 71 % and 24 to 88% yields,
respectively. The final products 1(a-g) were synthesized in 31 to 91% yields and
completely characterized by Infrared Spectroscopy (FT-IR), High Resolution Mass
Sprectrometry (HRMS) and Nuclear Magnetic Resonance (NMR). The compounds
1(a-g) are being evaluted against Staphylococcus aureus and Escherichia coli through
Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration
(MBC). These derivatives 1(a-g) did not show antibacterial activity against E. coli.
