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合成新型吡咯和稠合吡咯作为抗真菌和抗菌剂。

Synthesis of novel pyrroles and fused pyrroles as antifungal and antibacterial agents.

机构信息

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Helwan, Cairo, Egypt.

Department of Chemistry, The state University of New York at Buffalo, New York, NY, USA.

出版信息

J Enzyme Inhib Med Chem. 2021 Dec;36(1):2183-2198. doi: 10.1080/14756366.2021.1984904.

Abstract

Pyrroles and its fused forms possess antimicrobial activities, they can easily interact with biomolecules of living systems. A series of substituted pyrroles, and its fused pyrimidines and triazines forms have been synthesised, all newly synthesised compound structures were confirmed by spectroscopic analysis. Generally, the compounds inhibited growth of some important human pathogens, the best effect was given by: on Gram-positive bacteria and was higher on yeast (s), by on Gram-negative bacteria and by on filamentous fungi and ). Such results present good antibacterial and antifungal potential candidates to help overcome the global problem of antibiotic resistance and opportunistic infections outbreak. Compound gave the best anti-phytopathogenic effect at a 50-fold lower concentration than Kocide 2000, introducing a safe commercial candidate for agricultural use. The effect of the compounds on DNA was monitored to detect the mode of action.

摘要

吡咯及其稠合形式具有抗菌活性,它们可以很容易地与生物体系的生物分子相互作用。已经合成了一系列取代的吡咯,以及其稠合的嘧啶和三嗪形式,所有新合成的化合物结构都通过光谱分析得到了证实。一般来说,这些化合物抑制了一些重要的人类病原体的生长,效果最好的是:对革兰氏阳性菌,对酵母的效果更高,对革兰氏阴性菌的效果是 ,对丝状真菌的效果是 。这些结果表明,这些化合物具有良好的抗菌和抗真菌潜力,有助于克服抗生素耐药性和机会性感染爆发这一全球性问题。化合物在 50 倍的低浓度下给出了最好的抗植物病原效果,比 Kocide 2000 更安全,是一种有商业应用前景的候选农药。还监测了化合物对 DNA 的作用,以检测其作用模式。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d177/8491725/1408c9c1dbce/IENZ_A_1984904_SCH0001_C.jpg

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