Evranos AksÖz Begüm, GÜrpinar Suna Sibel, Eryilmaz Müjde
Süleyman Demirel University Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Isparta, Turkey.
Ankara University Faculty of Pharmacy, Department of Pharmaceutical Microbiology, Ankara, Turkey.
Turk J Pharm Sci. 2020 Oct;17(5):500-505. doi: 10.4274/tjps.galenos.2019.42650. Epub 2020 Oct 30.
Resistance to antibiotics is recognized as one of the biggest threats to human health worldwide. Frequent and unnecessary use of antibiotics has caused infectious agents to adapt to antibiotics and thus drugs have become less effective. The resistance to many antibiotics necessitates the discovery of new antibiotics. In this study, two new and 23 previously reported 2-pyrazoline derivatives and one hydrazone derivative were evaluated for their in vitro antibacterial and antifungal activities.
For the determination of the minimum inhibitory concentration (MIC) values of compounds, microbroth dilution was used.
The antimicrobial activities of the compounds were found in a wide range with MIC values of 32-512 μg/mL.
The synthesized compounds showed moderate antimicrobial activity compared with the standards. They can be used as lead molecules for the synthesis of more effective compounds.
抗生素耐药性被认为是全球人类健康面临的最大威胁之一。频繁且不必要地使用抗生素已导致感染病原体对抗生素产生适应性,从而使药物效果降低。对多种抗生素的耐药性使得发现新抗生素成为必要。在本研究中,对两种新型以及23种先前报道的2 - 吡唑啉衍生物和一种腙衍生物的体外抗菌和抗真菌活性进行了评估。
采用微量肉汤稀释法测定化合物的最低抑菌浓度(MIC)值。
化合物的抗菌活性范围较广,MIC值为32 - 512μg/mL。
与标准品相比,合成的化合物表现出中等抗菌活性。它们可作为合成更有效化合物的先导分子。