118030-33-4Relevant academic research and scientific papers
Pyrazolone derivatives: Synthesis, anti-inflammatory, analgesic quantitative structure-activity relationship and in vitro studies
Ragab, Fatma Abdel-Fattah,Abdel-Gawad, Nagwa Mohamed,Georgey, Hanan Hanna,Said, Mona Fikry
, p. 834 - 845 (2013/09/12)
Some 1-(4-chlorophenyl or benzenesulfonamide)-2,3- and/or 4-substituted-1H-pyrazol-5(4H)-one derivatives were synthesized and screened for their anti-inflammatory and analgesic activities, in addition to their ulcerogenic liability. They were found to be active as anti-inflammatory and analgesic agents. Compound 6b was found to be the most active as anti-inflammatory agent and compound 9b was found to be the most active one as anti-inflammatory and analgesic agent. On the other hand, cyclooxygenase-1/-2 (COX-1)/COX-2 isozyme selectivity was also done and the tested compounds showed equal inhibition to both isoforms. Moreover, 2D-quantitative structure-activity relationship (QSAR) studies revealed well predictive and statistically significant and cross validated QSAR model that helps to explore some expectedly potent compounds.
Synthesis, biological evaluation, and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis: Part 2. Synthesis of rigid pyrazolones
Castagnolo, Daniele,Manetti, Fabrizio,Radi, Marco,Bechi, Beatrice,Pagano, Mafalda,De Logu, Alessandro,Meleddu, Rita,Saddi, Manuela,Botta, Maurizio
scheme or table, p. 5716 - 5721 (2009/12/09)
Two series of novel rigid pyrazolone derivatives were synthesized and evaluated as inhibitors of Mycobacterium tuberculosis (MTB), the causative agent of tuberculosis. Two of these compounds showed a high activity against MTB (MIC = 4 μg/mL). The newly sy
