Synthesis and pharmacological investigation of 3-subsituted-amino-2-methylsulfanyl-5,6,7,8-tetrahydro-3H-benzo[4,5]thieno[2,3-d]pyrimidin-4-ones as analgesic and anti-inflammatory agents

被引:7
作者
Alagarsamy, V.
Solomon, V. Raja
Deepa, G.
Parthiban, P.
Anjana, G. V.
机构
[1] Dayananda Sagar Coll Pharm, Med Chem Res Lab, Bangalore 560078, Karnataka, India
[2] Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
[3] Arulmigu Kalasalingam Coll Pharm, Med Chem Res Lab, Anand, Krishnankovil, India
关键词
analgesic; anti-inflammatory activity; thienopyrimidin-4-one;
D O I
10.1002/ardp.200700017
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In the present work, design, synthesis, and pharmacological evaluation of the analgesic, antiinflammatory, and ulcerogenic-index activities of new 3-subsituted-amino-2-methylsulfanyl5,6,7,8-tetrahydro-3H-benzo[4,5]thieno[2,3-dlpyrimidin-4-ones, structurally planed by exploiting a clear concept of bio-isosterism, are reported. All compounds exhibited significant analgesic and anti-inflammatory activity. Compounds Al, A3 showed higher analgesic activity and more potent anti-inflammatory activity than that of the reference compound diclofenac sodium. Interestingly, the test compounds showed only mild ulcerogenic potential when compared to that of acetylsalicylic acid.
引用
收藏
页码:352 / 358
页数:7
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