Synthesis and Antifungal Activity Against of Candida Species for Some New Heterocyclic Compounds Containing Schiff Base , Oxazepine , Indoline or Imidazolo Units and Their Spectral Characterization

Shaima Ibrahim Chyad Al-khazraji, B. Mohammed, S. AL-Salihi
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引用次数: 1

Abstract

The objective of this study is to test In Vitro the twenty chemical compounds that contains Schiff base or oxazepine, indoline, imidazolo units in concentrations( 50, 100, 150) mg / dl as antifungal activity, against three pathogenic Candida species  that occur in humans. We tested one isolates of    ) Candida albicans ,Candida glabrata and Candida krusei). All these species affect human health . The study was carried out in the Laboratory of Public Health , directly of health for the period from May 2016 to April 2017  , Candida spp isolates used in this study were collected from patients admitted at  some private clinical in  Kirkuk city . All isolates were identified using CHROM agar and stored at -70 0C. Preparation of Schiff base ( 1-7 ) from amino pyridine derivatives with aromatic aldehyde by nucleophilic addition reactions preparation of 1,3 – oxazepine 4,7 – dione ( 8-13 ) were carried out by cyclization of appropriate Schiff bases with malic anhydride and phthalic anhydride , preparation of compounds ( 14 – 17) from reaction of a mixture aminopyridine derivative with potassium hydroxide then chloroacetic acid was  added , preparation of compounds ( 18 – 20 ) from reaction of amino pyridine derivative and 4- phenyl phenacyl bromide , all these compounds were characterized by melting points and FT.IR spectroscopy. Some of them were characterized by H1- NMR and C13-NMR spectroscopy .Some compounds contain Schiff base  group in compounds ( 1-7) showed inhibitory effect Candida albicans and Candida krusei  .This study demonstrates that the three Candida species were resistant to a range of compounds (8-13) containing oxazepine and as antifungal against , while the compound(14-17) contain Indolin show low inhabition zon for Candida albicans and the compound (18-20) contain imidazo group showed inhibited  effect against three Candida species.
希夫碱、恶西平、吲哚啉或咪唑类杂环化合物的合成及对念珠菌的抑菌活性研究
本研究的目的是在体外测试20种含有希夫碱或恶氮平、吲哚啉、咪唑啉单位浓度(50、100、150)mg / dl的化合物对三种人类致病性念珠菌的抗真菌活性。我们检测了一株白色念珠菌、光秃念珠菌和克鲁氏念珠菌。所有这些物种都会影响人类健康。该研究于2016年5月至2017年4月在公共卫生实验室进行,研究中使用的念珠菌分离株来自基尔库克市一些私人诊所收治的患者。所有分离株均采用CHROM琼脂进行鉴定,保存于-70℃。通过亲核加成反应由氨基吡啶衍生物与芳香醛合成席夫碱(1-7),通过适当的席夫碱与苹果酸酐和邻苯二甲酸酐环化制备1,3 -恶氮平4,7 -二酮(8-13),由氨基吡啶衍生物与氢氧化钾混合反应制备化合物(14 - 17),然后加入氯乙酸。以氨基吡啶衍生物和4-苯基苯那基溴为原料,制备了化合物(18 ~ 20),并用熔点和红外光谱对化合物进行了表征。部分化合物(1 ~ 7)中含有希夫碱基团,对白色念珠菌和克鲁氏念珠菌具有抑制作用。研究表明,这3种念珠菌对一系列含恶氮平的化合物(8 ~ 13)均具有抗真菌作用。含有吲哚啉组的化合物(14 ~ 17)对白色念珠菌呈低栖区,含有咪唑组的化合物(18 ~ 20)对3种念珠菌均有抑制作用。
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