Synthesis and antimicrobial evaluation of new 2-pyridinone and 2-iminochromene derivatives containing morpholine moiety,Journal of Heterocyclic Chemistry

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Synthesis and antimicrobial evaluation of new 2-pyridinone and 2-iminochromene derivatives containing morpholine moiety
Journal of Heterocyclic Chemistry ( IF 2.0 ) Pub Date : 2021-06-28 , DOI: 10.1002/jhet.4335
Mohamed A. Salem _{1,

2} , Samir Y. Abbas ₃ , Mohamed H. Hela ₄ , Abdullah Y. Alzahrani ₁

Affiliation

As trail to overcome on the antimicrobial drug-resistance problems, new functionalized 2-pyridinone and 2-iminochromene derivatives bearing morpholine moiety were designed and synthesized. The 2-pyridinone derivatives were obtained through the cyclization of cyanoacetohydrazone of 4-morpholinylacetophenone with 1,3-dicarbonyl compounds, α,β-unsaturated nitriles or 2-(arylidene)malononitriles. The 2-iminochromene derivatives were synthesized through the ring closure of cyanoacetohydrazonewith salicylaldehyde derivatives. The antibacterial and antifungal activities for the synthesized 2-pyridinone and 2-iminochromene derivatives were investigated. Most of the tested compounds showed moderate activity against P. vulgaris. Compounds 4a,b and 5a,b showed moderate activity against G −ve bacteria. All iminochromene derivatives showed moderate activity against C. albicans. Compound 8c was the most active compound.

中文翻译：

含有吗啉部分的新型 2-吡啶酮和 2-亚氨基色烯衍生物的合成和抗菌评价

为了克服抗微生物药物耐药性问题，设计并合成了新的功能化的 2-吡啶酮和 2-亚氨基色烯衍生物，它们带有吗啉部分。2-吡啶酮衍生物是通过4-吗啉基苯乙酮的氰基乙酰腙与1,3-二羰基化合物、α , β-不饱和腈或2-(亚芳基)丙二腈环化得到的。2-亚氨基色烯衍生物是通过氰基乙酰腙与水杨醛衍生物的闭环合成的。研究了合成的 2-吡啶酮和 2-亚氨基色烯衍生物的抗菌和抗真菌活性。大多数测试化合物对P表现出中等活性。寻常的。化合物4a,b和5a,b显示出对 G -ve 细菌的中等活性。所有亚氨基色烯衍生物均显示出对C 的中等活性。白种人。化合物8c是活性最强的化合物。

更新日期：2021-06-28

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