Synthesized Pyrazole Derivatives Research Articles

Carcinogenic effects of N-nitroso-3-(substituted phenylimino)-indolin-2-one derivatives.

Aim:A novel series of N-nitroso-3-(substituted phenylimino)-indolin-2-one 3a–h was synthesized and tested for carcinogenic effects.Materials and Methods:The synthesized pyrazole derivatives’ chemical structures were proved by means of their infra red (IR), proton nuclear magnetic resonance (1H-NMR), and mass,and confirmed by elemental analyses. The carcinogenic activity was assessed by 3–(4,5dimethyl thiazole–2yl)–2,5–diphenyltetrazoliumbromide (MTT) cell-viability assay.Results:The results show that most of the synthesized compounds exhibit significant carcinogenic activities. Among the synthesized compounds, N-nitroso-3-(2,4-dinitrophenylimino)-indolin-2-one 3h exhibited the most potent carcinogenic activity.Conclusion:The structure–activity relationship (SAR) studies show that the nature as well as the position of the amine are important for deciding the activity profile of the indolin-2-one derivatives, which reiterates the need for further experimental investigations.

Synthesis and antibacterial activity of a novel series of potent DNA gyrase inhibitors. Pyrazole derivatives.

We have previously found that a pyrazole derivative 1 possesses antibacterial activity and inhibitory activity against DNA gyrase and topoisomerase IV. Here, we synthesized new pyrazole derivatives and found that 5-[(E)-2-(5-chloroindol-3-yl)vinyl]pyrazole 16 possesses potent antibacterial activity and selective inhibitory activity against bacterial topoisomerases. Many of the synthesized pyrazole derivatives were potent against clinically isolated quinolone- or coumarin-resistant Gram-positive strains and had minimal inhibitory concentration values against these strains equivalent to those against susceptible strains.

The effects of newly synthesized pyrazole derivatives on formaldehyde-, carrageenan-, and dextran-induced acute paw edema in rats.

The antiinflammatory effects of 10 newly synthesized pyrazole derivatives on formaldehyde-induced rat paw edema were investigated. The most effective of them (K-3) was investigated again in dextran- and carrageenan-induced paw edema. In formaldehyde-induced paw edema, K-3 50, 100, and 200 mg/kg p.o. inhibited the edema by 48.9% (p<0.002), 68.7% (p<0.001), and 79.1% (p<0.001), respectively, 3 h after administration. In dextran-induced paw edema, the same dose of K-3 produced 27.1% (p<0.05), 46.8% (p<0.01), and 63.8% (p<0.002) inhibition, respectively. In the carrageenan-induced paw edema test, K-3 100 mg/kg decreased the inflammatory response by 52.0% after 4 h. Acute toxicity studies revealed that K-3 was nontoxic up to an oral dose of 2500 mg/kg.

Thin Layer Chromatographic Studies of Some Sulpha Drugs Substituted Pyrazoles Using Silica Gel-G Plates Impregnated with Various Adsorbents

Abstract Present communication describes the resolution of some Sulpha drugs substituted synthesized pyrazole derivatives on Silica gel-G plates impregnated with various adsorbents viz; sodium lauryl sulphate, Tetra ethyl ammonium perchlorate, Tetrabutyl ammonium bromide, Tetrabutyl ammonium hydroxide and Triton X-100.