Analgesic, anti-inflammatory, antipyretic and toxicological evaluation of some newer 3-methyl pyrazolone derivatives

Abstract

In this paper, we described the pharmacological and toxicological studies of three pyrazolone derivatives namely PYZ1: 4-[4-N dimethylamino benzylidine]-3-methyl pyrazolin-5(4H)-one, PYZ2: 4-[2-chlorobenzylidine]-3-methylpyrazolin-5(4H)-one and PYZ3: 4-[benzylidine]-3-methylpyrazolin-5(4H)-one derivatives. Analgesic, anti-inflammatory and antipyretic studies of 3-methyl pyrazolone derivatives at 400 mg/kg, p.o. have shown significant activity as compared to control. Amongst three pyrazolone derivatives, PYZ2 was found to be more active. Based on the result of pharmacological studies, PYZ2 was selected for toxicological studies. Acute toxicity studies revealed that methyl pyrazolone derivatives are non-toxic in rats up to 5000 mg/kg, p.o. The subacute toxicity study of PYZ2 showed that decrease in Hb content, RBC and WBC count. In biochemical analysis level of blood glucose and bilirubin reduced where as AST, ALT and alkaline phosphatase level elevated. Histopathological studies revealed that there was mild toxicity on liver and kidney at 1000 mg/kg, p.o.

Synthesis and Isolation of 2,9,17,23-Tetrakis[(3,5-dimethyl-1H-pyrazol-1-yl)phenoxy]phthalocyanine and Its Magnesium(II) and Zinc(II) Complexes

“…[28,29] However, only a few works devoted to phthalocyanines [30][31][32] and porphyrin [33] containing pyrazole substituents are known. Interest to such substituents is caused by various biological activity of the pyrazole derivatives (antimicrobial, [34] antipyretic, [35] analgesic, [36] anti-inflammatory, [37] antiviral [38] and other properties [39] ). The high singlet oxygen quantum yield of zinc phthalocyanine containing four 3,5-dimethylpyrazole-1-methoxy groups gives an indication of the potential of the zinc phthalocyanine as photosensitizer in photocatalytic applications such as PDT.…”

Cytotoxicity and Oral Acute Toxicity Studies of b-mangostin Isolated from Cratoxylum arborescens

“…The transaminases (AST and ALT) are well-known enzymes which are good indicators of liver function as biomarkers in predicting toxicity. [27] Any kind of insult to the parenchymal liver cells results elevated level of both transaminases in the blood. [28] The serum AST is of both mitochondrial and cytoplasmic origin and hence any rise of its level is considered first sign of cell damage that leads to the outflow of the enzymes into the serum.…”

Synthesis of 4-(4-hydrazinylphenoxy)phthalonitrile and phthalonitriles on its basis containing N-heterocycles

“…These substituents are attached to a linked phthalocyanine macroheterocycle directly, [16] through the methoxy spacer moiety [17] or through oxygen atom spacer moiety. [18] Interest to such substituents is caused by various biological activity of the pyrazole derivatives (antimicrobial, [19] antipyretic, [20] analgesic, [21] antiinflammatory, [22] antiviral [23] properties and others [24] ). It is known that effective method for synthesis of substituted phthalocyanines is based on the corresponding phthalonitriles.…”