Synthesis of novel 1,3,4-trisubstituted pyrazoles as anti-inflammatory and analgesic agents
Synthesis of novel 1,3,4-trisubstituted pyrazoles as anti-inflammatory and analgesic agents
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DOI：
10.1016/j.ejmech.2013.03.005
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发表时间：
2013-05-01
影响因子：
6.7
通讯作者：
Said, Mona F.
中科院分区：
文献类型：
--
作者：
Ragab, Fatma A.;Gawad, Nagwa M. Abdel;Said, Mona F.
合成了一些新的1，3，4-三取代吡唑类化合物，并对其抗炎、镇痛和致溃疡活性进行了筛选。它们表现出抗炎和镇痛活性，具有比标准药物保泰松更好的GIT耐受性。此外，记录了5e和8 e的IC 50值。化合物5e是最具抗炎镇痛活性的化合物。另一方面，还进行了考克斯-1/考克斯-2同工酶选择性，其显示对两种同工型的相等抑制。(c)2013年Elsevier Masson SAS。All rights reserved.
Some novel 1,3,4-trisubstituted pyrazoles were synthesized and screened for their anti-inflammatory and analgesic activities as well as their ulcerogenic liability. They showed anti-inflammatory and analgesic activities with better GIT tolerance than the standard drug phenylbutazone. In addition, IC50 values for 5e and 8e were recorded. Compound 5e was found to be the most active one as anti-inflammatory and analgesic agent. On the other hand, COX-1/COX-2 isozyme selectivity was also done which showed equal inhibition to both isoforms. (c) 2013 Elsevier Masson SAS. All rights reserved.