NOVEL SYNTHESIS OF PYRAZOLE-CONTAINING THIOPHENE, 2-ALKYLOXY-PYRIDINE AND THIENO[2,3-d]PYRIMIDINE SCAFFOLDS AS ANALGESIC AGENTS

被引:4
作者
Khalifa, Nagy M. [1 ,2 ]
Fahmy, Hoda H. [2 ]
Nossier, Eman S. [3 ]
Amr, Abd El-Galil E. [4 ]
Herqash, Rashed N. [5 ]
机构
[1] King Saud Univ, Coll Pharm, Pharmaceut Chem Dept, Drug Explorat & Dev Chair DEDC, Riyadh 11451, Saudi Arabia
[2] Natl Res Ctr, Therapeut Chem Dept, Pharmaceut & Drug Ind Div, Giza, Egypt
[3] Al Azhar Univ Girls, Fac Pharm, Pharmaceut Chem Dept, Cairo, Egypt
[4] Natl Res Ctr, Appl Organ Chem Dept, Giza 12622, Egypt
[5] King Saud Univ, Coll Pharm, Pharmaceut Chem Dept, Riyadh 11451, Saudi Arabia
关键词
Trisubstituted pyrazoles; Thiophene; Alkyloxypyridine; Fused pyrimidine; Analgesic activities; BIOLOGICAL EVALUATION; DERIVATIVES; DESIGN; INHIBITION; DOCKING; ANALOGS; SAR;
D O I
10.4314/bcse.v33i3.11
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A group of trisubstituted pyrazoles containing thiophen, 2-alkyloxypyridine and thieno[2,3-d]pyrimidine heterocycles were synthesized in a study for possible analgesic agents. The desired products were obtained by reaction of 2-(1-(3-chlorophenyl)-3-(4-methoxyphenyl)-1H-pyrazol-4-yemethylene)malononitrile with sulfur in presence of TEA, followed by treatment with different reagents. Newer products were examined for their analgesic properties, among them, analog 7 showed significant analgesic effects in comparison with reference medicines activity.
引用
收藏
页码:505 / 515
页数:11
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