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一种在乙酸介质中合成新型甲基砜的有效方法及抗菌活性评估。

An efficient approach for the synthesis of novel methyl sulfones in acetic acid medium and evaluation of antimicrobial activity.

作者信息

Ravi Kumar Gollapudi, Dasireddy Chandra Rao, Varala Ravi, Kotra Vijay, Bollikolla Hari Babu

机构信息

Department of Chemistry, Acharya Nagarjuna University, Guntur, Andhra Pradesh India.

Department of Chemistry, Government Degree College, Husnabad, Telangana India.

出版信息

Turk J Chem. 2020 Oct 26;44(5):1386-1394. doi: 10.3906/kim-2003-10. eCollection 2020.

Abstract

A series of nine methyl sulphones ( -3 ) starting from the aldehydes ( ) were synthesized in two consecutive steps. In the first step, preparation of allyl alcohols ( ) from their corresponding aldehydes by the reaction of sodium borohydride in methanol at room temperature is reported. Finally, methyl sulphones are synthesized by condensing sodium methyl sulfinates with allyl alcohols in the presence of BF .Et O in acetic acid medium at room temperature for about 2-3 h. The reaction conditions are simple, yields are high (85%-95%), and the products were obtained with good purity. All the synthesized compounds were characterized by their H, C NMR, and mass spectral analysis. All the title compounds were screened for antimicrobial activity. Among the compounds tested, the compound has inhibited both Gram positive and Gram negative bacteria effectively and compound has shown potent antifungal activity. These promising components may help to develop more potent drugs in the near future for the treatment of bacterial and fungal infections.

摘要

从醛类化合物( )出发,通过两个连续步骤合成了一系列九种甲基砜( -3 )。第一步,报道了在室温下,通过硼氢化钠在甲醇中与相应醛类反应制备烯丙醇( )。最后,在室温下,于乙酸介质中,在BF .Et O存在下,通过亚磺酸钠与烯丙醇缩合约2 - 3小时来合成甲基砜。反应条件简单,产率高(85% - 95%),且产物纯度良好。所有合成化合物均通过 H、 C NMR和质谱分析进行了表征。对所有标题化合物进行了抗菌活性筛选。在所测试的化合物中,化合物 对革兰氏阳性菌和革兰氏阴性菌均有有效抑制作用,化合物 显示出强效抗真菌活性。这些有前景的成分可能有助于在不久的将来开发出更有效的治疗细菌和真菌感染的药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/92da/7751907/50aa9ec9a89a/turkjchem-44-1386-sch001.jpg

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