微波辅助合成连接嘧啶部分的新型吡唑酮衍生物及其抗炎、镇痛和退热活性评价。
Microwave assisted synthesis of novel pyrazolone derivatives attached to a pyrimidine moiety and evaluation of their anti-inflammatory, analgesic and antipyretic activities.
机构信息
Medicinal Chemistry Research Laboratory, Acharya & B.M. Reddy College of Pharmacy, Bangalore 560 090, Karnataka, India.
出版信息
Saudi Pharm J. 2011 Oct;19(4):233-43. doi: 10.1016/j.jsps.2011.05.006. Epub 2011 Jun 25.
Abstract
In the present research work, the motto was to develop new chemical entities as potential anti-inflammatory, analgesic and antipyretic agents. Various 4-(2-amino-6-(substituted)pyrimidin-4-yl)-3-methyl-1-(substituted)-1H-pyrazol-5(4H)-one derivatives (5a-5j) and their Schiff bases (6a-6j) were synthesized. The newly synthesized compounds were characterized by TLC and spectral data. The compounds containing pyrazolone and amino pyrimidine as basic moieties (5a-5j), were screened for their anti-inflammatory, analgesic and antipyretic activities, compounds 5a, 5c-5f, 5h exhibited activities nearly similar to the standard. The pharmacological studies reveal that the presence of 4-hydroxy, 4-methoxy, 4-(N,N-dimethylamino) or 2-hydroxy groups on phenyl ring at C6 of amino pyrimidine exhibits anti-inflammatory, analgesic and antipyretic activities nearly similar to the standard and substitutions like 4-chloro, 2-nitro, 3-nitro or 4-nitro on same phenyl ring lead to a decrease in activities.
摘要
在本研究工作中，我们的宗旨是开发新的化学实体，作为潜在的抗炎、镇痛和退热剂。各种 4-(2-氨基-6-(取代)嘧啶-4-基)-3-甲基-1-(取代)-1H-吡唑-5(4H)-酮衍生物 (5a-5j) 和它们的席夫碱 (6a-6j) 被合成了。新合成的化合物通过 TLC 和光谱数据进行了表征。含有吡唑酮和氨基嘧啶作为基本部分的化合物 (5a-5j) 被筛选其抗炎、镇痛和退热活性，化合物 5a、5c-5f、5h 表现出与标准品相似的活性。药理学研究表明，氨基嘧啶 C6 上苯基环上的 4-羟基、4-甲氧基、4-(N,N-二甲基氨基)或 2-羟基的存在表现出与标准品相似的抗炎、镇痛和退热活性，而在同一苯基环上的 4-氯、2-硝基、3-硝基或 4-硝基等取代基会导致活性降低。
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