Alguns novos derivados de pirazol-5-carbonitrila 8,9 e pirazol-5-carboxamida 13 foram sintetizados pela reação de cicloadição de nitriliminas 3,4 a α-cianocinamonitrilas 5a-f e α-cianocinamamida 12a,b, respectivamente. Por outro lado, a adição de 3,4 a α-cianocinamato de etila 14a-f leva à produção de derivados de 2-pyrazoline-5-carboxilato de etila, 15, 16. Também, a cicloadição de 3,4 à 3-cia...

The ability of several N-phenyl-1H-pyrazole-4-carboxamide derivatives and other pyrazoles opportunely modified at the positions 3, 4 and 5, to reduce the formation of the biofilm in some Staphylococcus aureus strains (ATCC 29213, ATCC 25923 and ATCC 6538) were investigated. All the tested compounds were able, although to a different extent, to reduce the biofilm formation of the three bacterial...

In search of synthetic chemotherapeutic substances capable of inhibiting, retarding, or reversing the process of multi-stage carcinogenesis, we synthesized a series of novel 5-amino pyrazole derivatives 11(a-h) by a nucleophilic substitution reaction and characterized by H nuclear magnetic resonance (NMR), liquid chromatography mass spectrometry (LC/MS), Fourier-transform infrared (FTIR), and e...

An organocatalyzed Michael-cyclization cascade approach of readily available α,β-unsaturated aldehydes and pyrazoleamides has been developed to get highly substituted δ-lactones in excellent enantioselectivities (up to 97%) and diastereoselectivities. The δ-lactones so obtained could easily be transformed into benzazepine derivatives with excellent enantio- and diastereoselectivities. Furthermo...

Novel tetrasubstituted pyrazole derivatives bearing a nitro substituent on their A-phenol ring were synthesized and their binding affinity towards the estrogen receptor (ER) subtypes ERalpha and ERbeta was determined. Among compounds tested, the 2-nitrophenol derivative 5c was found to bind satisfactorily to both estrogen receptor subtypes (RBAalpha=5.17 and RBAbeta=3.27). In general, the intro...