Antifungal activity, SAR and physicochemical correlation of some thiazole-1,3,5-triazine derivatives

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• 作者：U.P. Singh^a ; ^{udaysingh98@gmail.com} ; H.R. Bhat^a ; P. Gahtori^b
• 关键词：1 ; 3 ; 5-triazine ; Antifungal activity ; SAR ; Physicochemical property
• 刊名：Journal de Mycologie M&eacute ; dicale / Journal of Medical Mycology
• 出版年：2012
• 期刊代码：156_11565233
• 类别：med
• 出版时间：June, 2012
• 卷：22
• 期：2
• 页码：134-141
• 文件大小：578 K

摘要

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class="h3">Summary

class="h4">Objective

Present research communication was towards the investigation of antifungal minimum inhibitory concentration (MIC) and minimum fingicidal concentration (MFC) activity of some substituted clubbed thiazole-1,3,5-triazines derivatives and effect of physicochemical properties on bioactivity.

class="h4">Material and methods

MIC and MFC were evaluated against Candida albicans, Candida glabrata, Cryptococcus neoformans and Aspergillus niger using modified microdilution method recommended by CLSI. Cytotoxicity was determinate on the viability of marine shrimp larvaes. SAR and physicochemical correlations were studied by Molinspiration software.

class="h4">Results

The class="boldFont">5 and class="boldFont">9 derivatives showed an excellent antifungal activity with MIC lower than fluconazole and equivalent to amphotericin B specially against C.聽albicans and C.聽glabrata. The toxicity of these two derivatives was non-existent for class="boldFont">5 and moderate for class="boldFont">9 at the used concentration. SAR study around prototype molecule suggests that presence of di-hydrophobic fragment on 1,3,5-triazine is necessary for antifungal activity than halogen substituted aromatic amine.

class="h4">Conclusion

On the basis of selectivity, potency and non-toxicity, we have obtained two molecules (5 and 9) as prospective leads for further research work on 1,3,5-triazine as antifungal drug.