European Journal of Molecular & Clinical Medicine

Pharmacological screening of Euphorbia Neriifolia Linn. (Euphorbiaceous) leaf hydro alcoholic extract were performed to explore anti-ulcer activities. All tests were conducted on rats using 100, 200 and 400mg/kg dose as LD so of extract was found to 2779.71mg/kg. Study revealed strong analgesic effect of E. Neriifolia against thermal (P<0.001), and in mechanical and chemical (p < 0.01) noxious stimuli and anti-inflammatory activity (P<0.001 to 0.01) at the 1000mg/kg dose. In camageen an-induced paw edema and cotton pellet induced granuloma model. Neriifolia extract showed significant (P<0.001 to 0.01) anti- inflammatory activity. Extract considerably increases urine volume as an effective hypermatraemic and hyperchloraemic diuretic. E. Neriifolia showed laxative property by increasing wet defecation along with castor oil. Extract showed very prominent protection against ethanol-induced ulceration as well as on pyloric ligated ulceration in dose dependent manner. Extract increases total hexodes (P<0.001), Hexosamine (P<0.05), Sialic acid and total carbohydrate content (P<0.001) with a decrease in total protein content (P<0.001) of gastric mucosa at 400mg/kg dose. Presence of Phytoconstituents like tannins, flavonoids, alkaloids and triterpenoidal saponins may be responsible for the found pharmacological activities.

Pyrazolopyrimidines and related fused heterocycles are of interest as potential bioactive molecules. The heterocyclic fusion of pyrimidine ring and pyrazole ring resulted in formation of pyrazolopyrimidines, the structural analogues of biogenic purine class, undoubtedly, has high significance in the field of pharmaceutical and biotechnological sciences with wide spectrum of biological activities and its several derivatives. Toxicity may be due to the accumulation in a specific organ/ tissue (e.g. bosentan), the co -administration of other drugs affecting ADMET (absorption, distribution, metabolism, elimination and toxicity) Cmax reaching off target IC50, or the high Cmax required for therapeutic effects. Assessing the relative drug efficacy and toxicity is important for medicinal chemists, pharmacologists, pharmacists, physicians. As multiple treatment options are available for many diseases, relative toxicity assessment is necessary. Difficulty in direct clinical trial comparisons forces network meta-analyses for estimating the relative toxicity. Therapeutic index (TI) assumes simplified linear relationships between receptor affinity, maximum unbound plasma drug concentration (Cmax) and toxicity. But high TI does not guarantee safety. For drugs metabolized by cytochrome P450 (CYP450),estimating TI based on target potencies alone is insufficient.

The key objective of the current research is to synthesize and analgesic action 5- (2-(2,3-dimethylphenylamino)phenyl)-2-(aryl)- 1,3,4-oxadiazole and to test this activity (VT1- VT8). During this investigation, the condensed methanone {2-[(2,3- dimethylphenyl)amino]phenyl}(hydrazinyloxide), and various aryl-acids in presence of phosphorous oxychloride were synthesized in the present investigations by a sequence of 5-(2- (2,3-dimethylphenylamino)phenyl]-2,3,4-oxadiazols (VT1-VT8). Both synthesized compounds have been tested with 50 mg/kg and 10 mg/kg po respectively for their in vivo antiinflammatory and analgesic activities. Carrageen's mediated acute rat paw oedema model and Eddy's hot plate system were used to analyze the anti-inflammatory and analgesic function of the synthesized compounds. Any substances have been effective at their anti-inflammatory and analgesic activities, according to biological results. Elemental research (C, H, N) and spectral analysis also verified the composition of both substances (IR, 1H NMR and mass spectrometry).