Online ISSN: 2515-8260

Keywords : Anti-inflammatory activity

Synthesis Of Pyrazolopyrimidine Derivatives Along With Its Biological Activity Including Toxicity Studies

S. Singh; Dr. Mohammad. Gousuddin; Huma Khan

European Journal of Molecular & Clinical Medicine, 2021, Volume 8, Issue 2, Pages 182-200

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.


Vishal kumar; Satish Kumar Sharma; Rizwan Ahmad

European Journal of Molecular & Clinical Medicine, 2020, Volume 7, Issue 1, Pages 4406-4415

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).