New hydrazide-hydrazones of isonicotinic acid: synthesis, lipophilicity and in vitro antimicrobial screening

被引:30
作者
Popiolek, Lukasz [1 ]
Biernasiuk, Anna [2 ]
Berecka, Anna [3 ]
Gumieniczek, Anna [3 ]
Malm, Anna [2 ]
Wujec, Monika [1 ]
机构
[1] Med Univ Lublin, Dept Organ Chem, Fac Pharm, Lublin, Poland
[2] Med Univ Lublin, Dept Pharmaceut Microbiol, Fac Pharm, Lublin, Poland
[3] Med Univ Lublin, Dept Med Chem, Fac Pharm, Lublin, Poland
关键词
antibacterial activity; antifungal activity; hydrazide-hydrazone; MBC; MIC; ANTIMYCOBACTERIAL ACTIVITY; DERIVATIVES; DESIGN; DOCKING; ANALOGS; AGENTS;
D O I
10.1111/cbdd.13158
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
This study describes the synthesis, lipophilicity and in vitro antimicrobial assays of 15 new hydrazide-hydrazones of isonicotinic acid. New derivatives were obtained on the basis of the condensation reaction of isonicotinic acid hydrazide with different aromatic aldehydes. The chemical structure of synthesized compounds was confirmed by spectral methods. Experimental lipophilicity of new isonicotinic acid derivatives was determined using reversed-phase thin-layer chromatography. All synthesized compounds were subjected to in vitro antimicrobial assays against reference strains of Gram-positive bacteria, Gram-negative bacteria and fungi belonging to Candida spp. Some of the synthesized hydrazide-hydrazones proved to be significant antibacterial compounds and more potent than commonly used chemotherapeutic agents.
引用
收藏
页码:915 / 923
页数:9
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