Current status of pyrazole and its biological activities

Abstract

Pyrazole are potent medicinal scaffolds and exhibit a full spectrum of biological activities. This review throws light on the detailed synthetic approaches which have been applied for the synthesis of pyrazole. This has been followed by an in depth analysis of the pyrazole with respect to their medical significance. This follow-up may help the medicinal chemists to generate new leads possessing pyrazole nucleus with high efficacy.

(E)-Substituted-N-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)benzeneamine: synthesis, characterization, antibacterial, and MTT assessment

“…Series of fifteen (E)-Substituted-N-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)benzeneamine derivative (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15) was aimed for the synthesis, following the three step procedure (Fig. 1).…”

“…In the second step the Schiff bases undergoes cyclization to yield pyrazole carboxaldehyde (b1-b5) nucleus by using dimethylformamide (DMF) and the desired compounds (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15) by the condensation reaction between pyrazole carboxaldehyde (b1-b5) and substituted amines in ethanol and drop of acetic acid under reflux. The prepared derivatives (a1-a5), (b1-b5) and (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15) were then analyzed for structural confirmation by variety of analytical techniques such as FTIR, NMR, Mass Spectroscopy, Elemental analysis. The FTIR bands around 1590-1602 and 3190-3222 cm −1 due to the presence of C=N and NH functional groups confirmed the formation of compounds (a1-a5), the singlet around 1098-11.18 ppm in 1 H-NMR spectra due to the NH proton and a strong signal around 166.08-166.90 ppm in 13 C-NMR spectra due to C=N carbon further confirmed the formation of compounds (a1-a5).…”

“…Screening of the antimicrobial therapeutic effect of the synthesized compounds was carried out employing the disc diffusion method. The stock solution of the test compounds was prepared by dissolving one mg of each compound (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15) to the 100 mL of dimethysulphoxide (DMSO). The microbes [S. aureus (ATCC-25923), S. epidermidis (ATCC-29887), E. coli (ATCC-25922), P. mirabilis (ATCC-25933) were sub-cultured in nutrient agar media, following by the McFarland Protocol and transferred to the agar plate.…”

“…Pyrazole moiety has been found in some currently used chemotherapeutic agents like Rimonabant, Tapoxalin, Lonazolac, Pyrazofurin, Epirizole, Celecoxib and Fezolamine etc. [3]. The versatile therapeutic application of the pyrazole derivative have been reported such as antimicrobial [4], Antimalarial [5], anticancer [6], anti-inflammatory [7], antidepressant [8], anticonvulsant [9], selective enzyme inhibitory activities [10], antipyretic [11], analgesic [12], fungicidal [13], fungistatic [14], antihyperglycemic [15], antiviral [16], antitumor [16], etc.…”

Green synthesis of pyrazole systems under solvent-free conditions

“…In most of these methods, diverse organic solvents such as ethanol, toluene, CH 2 Cl 2 , acetone and acetonitrile have been used (22)(23)(24)(25)(26)(27)(28)(29)(30)(31). The obtained product yields of most of these reactions are significant, but the solvents used are not compatible with the environment or cost savings.…”