取代4-(溴乙基)- n-(4-乙基-6-甲基嘧啶-2-基)苯酰胺衍生物的合成、表征及抑菌活性评价

M. Laxmi, G. Ravi, A. Nath
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摘要

以取代4-乙基-6-甲基嘧啶-2-胺和4-(溴乙基)苯甲酰溴5为原料,在KOH存在下合成了取代4-(溴乙基)- n-(4-乙基-6-甲基嘧啶-2-基)苄酰胺衍生物6ak。醛和酮之间的醛缩反应类型,形成α,β-不饱和羰基化合物3。该化合物与胍在干醇存在下反应,转化为4-乙基-6 -甲基嘧啶-2-胺4。所有新化合物的化学结构均通过IR、1H、13C NMR、MS和元素数据确定。化合物6a-k对革兰氏阳性菌枯草芽孢杆菌、球形芽孢杆菌和金黄色葡萄球菌以及3种革兰氏阴性菌铜绿假单胞菌、产气克雷伯菌和紫色嗜铬杆菌的抑菌活性进行了评价,并对白色念珠菌(C.albicans)(ATCC 10231)、烟曲霉(A.fumigatus) (HIC 6094)、红毛癣菌(T。红藓属(IFO 9185)和毛藓属(T。其中含有[3-hydrophenyl] 6d、[3- chlorphenyl] 6f和[4-nitrophenyl] 6h的化合物具有显著的抗菌和抗真菌活性,几乎等于或超过标准药物Streptomycin和Amphotericin-B的活性。此外,对化合物6a-k也进行了筛选,大多数新化合物对测试细菌和真菌具有明显的活性,并成为进一步开发的潜在分子。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis, Characterization of substituted 4-(bromomethyl)-N-(4-ethyl-6-methylpyrimidin-2-yl)benzamide Derivatives and Evaluation of their Anti-microbial activity.
The substituted 4-(bromomethyl)-N-(4-ethyl-6-methylpyrimidin-2-yl) benzamide derivatives 6ak has been synthesis from reaction in between substituted 4-ethyl-6-methylpyrimidin-2-amine and 4-(bromomethyl)benzoyl bromide 5 in presence of KOH. Type of aldol condensation reaction in between aldehydes and ketones to form α,β-Unsaturated carbonyl compounds3 this compound has been reacted with guanidine in presence of dry alcohol to convert 4-ethyl-6methylpyrimidin-2-amine4.Chemical structures of all the new compounds were established by IR, 1H, 13C NMR, MS and elemental data. The compounds 6a-k were evaluated for their antibacterial activity against Gram-positive bacteria viz. Bacillus subtilis, Bacillus sphaericus and Staphylococcus aureus, and three Gram-negative bacteria viz. Pseudomonas aeruginosa, Klebsiella aerogenes and Chromobacterium violaceum and also evaluate their antifungal activity against Candida albicans (C.albicans)(ATCC 10231), Aspergillus fumigates(A.fumigatus) (HIC 6094), Trichophyton rubrum(T. rubrum) (IFO 9185), and Trichophyton mentagrophytes(T. mentagrophytes) (IFO 40996) Amongst them, compounds containing [3-hydrophenyl] moiety 6d, [3-chlorophenyl] moiety 6f and [4-nitrophenyl] moiety 6h showed significant antibacterial and antifungal activity, almost equal/more than the activity of the standard drugs Streptomycin and Amphotericin-B. Further, the compounds 6a-k were also screened for Most of these new compounds showed appreciable activity against test bacteria and fungi and emerged as potential molecules for further development.
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