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Synthesis and anti-microbial activity of some 1- substituted amino-4,6-dimethyl-2-oxo-pyridine-3-carbonitrile derivatives
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2011-08-25 , DOI: 10.1016/j.ejmech.2011.08.018
Rizk E. Khidre , Ameen A. Abu-Hashem , Mohamed El-Shazly

A new series of 1- substituted amino-4,6-dimethyl-2-oxo-pyridine-3-carbonitrile such as hydrazide hydrazones 3a-h; ethane-1,2-diaminopyridine 6; phthalimidopyridines 8a,b; hydrazides 10a,b; urea 11a and thiourea 11b were synthesized in a good to excellent yield in step efficient process, using 1-amino-4,6-dimethyl-2-oxo-1,2-dihydropyridine-3-carbonitrile (1) as a key intermediate. The antibacterial and antifungal activities of the synthesized compounds were evaluated. The obtained data indicated that the majority of the tested compounds exhibited both antibacterial and antifungal activities, particularly compounds 8a and 8b showed a comparable effect to a well known antibacterial and antifungal agents.



中文翻译:

一些1-取代的氨基-4,6-二甲基-2-氧代吡啶-3-甲腈衍生物的合成及抑菌活性

一类新的1-取代的氨基-4,6-二甲基-2-氧代吡啶-3-甲腈,如酰肼3a-h;乙烷-1,2-二氨基吡啶6 ; 邻苯二甲酰亚胺吡啶8ab ; 酰肼10ab ; 尿素11A和硫脲11B在一个良好的在步骤有效的方法高收率合成,使用1-氨基-4,6-二甲基-2-氧代-1,2-二氢吡啶-3-甲腈(1)作为关键中间体。评价了合成化合物的抗菌和抗真菌活性。获得的数据表明,大多数受试化合物均显示出抗菌和抗真菌活性,特别是化合物8a8b显示出与众所周知的抗菌和抗真菌剂相当的作用。

更新日期:2011-08-25
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