Synthesis of Some Novel Heterocycles Bearing Thiadiazoles as Potent Anti-inflammatory and Analgesic Agents

被引:20
|
作者
Gomha, Sobhi M. [1 ]
Muhammad, Zeinab A. [2 ]
Gaber, Hatem M. [2 ]
Amin, Mohamed M. [3 ]
机构
[1] Cairo Univ, Dept Chem, Fac Sci, Giza 12613, Egypt
[2] Natl Org Drug Control & Res NODCAR, POB 29, Cairo, Egypt
[3] Natl Res Ctr, Div Med, Dept Pharmacol, 33EL Bohouth St, Giza 12622, Egypt
关键词
PHARMACOLOGICAL EVALUATION; DERIVATIVES; THIAZOLES;
D O I
10.1002/jhet.2872
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
2-Bromoacetyl-3-phenyl-1,3,4-thiadiazole derivative was synthesized and reacted with a number of heterocyclic amines to give a series of fused imidazole derivatives. Also, reaction of 2-bromoacetyl-3-phenyl-1,3,4-thiadiazole with o-phenylene diamine and 2-aminothiophenol yielded the respective products. Moreover, reaction of 2-bromoacetyl-3-phenyl-1,3,4-thiadiazole with thiourea, thiosemicarbazide, thiocarbahydrazide gave the respective thiazoles. The structures of all the novel products were elucidated on the basis of elemental analysis and spectral data. In addition, the biological activity of the newly synthesized compounds was evaluated, and the results obtained indicate their potency as anti-inflammatory, analgesic, and anti-ulcer agents. The binding mechanism of the most active compounds was studied using MOE to analyze the molecular interactions.
引用
收藏
页码:2708 / 2716
页数:9
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