Halimehjani Azim Ziyaei, Dehghan Faezeh, Tafakori Vida, Amini Elaheh, Hooshmand Seyyed Emad, Nosood Yazdanbkhsh Lotfi
Faculty of Chemistry, Kharazmi University, 49 Mofateh St., 15719-14911, Tehran, Iran.
Department of Cell and Molecular Biology, Faculty of Biological Sciences, Kharazmi University, Tehran, Iran.
Heliyon. 2022 May 30;8(6):e09564. doi: 10.1016/j.heliyon.2022.e09564. eCollection 2022 Jun.
A metal-free multicomponent synthetic route for the diverse preparation of dithiocarbamate-containing piperazine derivatives was developed through the C-N bond cleavage of DABCO ring. This multicomponent re-engineering approach proceeds the reaction of amines, CS and DABCO salts in one pot. Various DABCO salts and secondary amines are tolerated well in this protocol to afford a broad spectrum of dithiocarbamate-containing piperazines in good to high yields. Then, the selected compounds have been deployed against some critical types of bacteria and fungi. A certain number of synthesized compounds revealed not only appropriate antibacterial activity as investigated by disc fusion and minimum inhibitory concentration methods against bacteria (Gram-positive and Gram-negative), but also depicted good to excellent antifungal activity.
通过1,4-二氮杂双环[2.2.2]辛烷(DABCO)环的C-N键裂解,开发了一种无金属多组分合成路线,用于多样地制备含二硫代氨基甲酸盐的哌嗪衍生物。这种多组分重新设计方法使胺、CS和DABCO盐在一锅反应中进行反应。各种DABCO盐和仲胺在该方案中耐受性良好,以良好至高产率得到了广泛的含二硫代氨基甲酸盐的哌嗪。然后,所选择的化合物已被用于对抗一些关键类型的细菌和真菌。通过纸片扩散法和最低抑菌浓度法对细菌(革兰氏阳性和革兰氏阴性)进行研究,一定数量的合成化合物不仅显示出适当的抗菌活性,而且还表现出良好至优异的抗真菌活性。