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Synthesis of New Bis-pyrazolines Endowed with Potent Antifungal Activity against Candida albicans and Aspergillus niger
Letters in Drug Design & Discovery ( IF 1 ) Pub Date : 2020-12-31 , DOI: 10.2174/1570180817999201008155247
Belgin Sever 1 , Mehlika Dilek Altintop 1 , Ahmet Özdemir 1
Affiliation  

Background: Due to the increasing number of cases of invasive fungal infections (IFIs), there is an urgent need to identify potent antifungal agents capable of combating IFIs. Pyrazolines are one such class of therapeutically active agents that could be considered to fulfill this need.

Objective: In this context, this paper aims to identify two new series of bis-pyrazolines endowed with potent antifungal activity against Candida albicans and Aspergillus niger.

Methods: Two new series of bis-pyrazolines (4a-i, 5a-e) were synthesized through an efficient and versatile synthetic procedure. The compounds were screened for their antifungal effects on C. albicans and A. niger using a broth microdilution method. Their cytotoxic effects on NIH/3T3 mouse embryonic fibroblast cells were determined using MTT assay. Molecular docking studies were performed in the active site of lanosterol 14



中文翻译:

具有对白色念珠菌黑曲霉的强抗真菌活性的新型双吡唑啉的合成

背景:由于侵袭性真菌感染(IFI)的病例数量不断增加,迫切需要确定能够与IFI对抗的有效抗真菌剂。吡唑啉是可以被认为满足这种需要的一类此类治疗活性剂。

目的:在此背景下,本文旨在确定两个新的双吡唑啉类,它们具有对白色念珠菌和黑曲霉的有效抗真菌活性。

方法:通过高效且通用的合成方法合成了两个新的双吡唑啉系列(4a-i,5a-e)。使用肉汤微稀释法筛选化合物对白色念珠菌和黑曲霉的抗真菌作用。用MTT法测定它们对NIH / 3T3小鼠胚胎成纤维细胞的细胞毒性作用。在羊毛甾醇14的活性位点进行了分子对接研究

更新日期:2021-02-26
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