title: Antifungal activity, SAR and physicochemical correlation of some thiazole-1,3,5-triazine derivatives.
abstract: OBJECTIVE
  Present research communication was towards the investigation of antifungal minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) activity of some substituted clubbed thiazole-1,3,5-triazines derivatives and effect of physicochemical properties on bioactivity.
  
  
  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.
  
  
  RESULTS
  The 5 and 9 derivatives showed an excellent antifungal activity with MIC lower than fluconazole and equivalent to amphotericin B specially against C. albicans and C. glabrata. The toxicity of these two derivatives was non-existent for 5 and moderate for 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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Department of Pharmaceutical Sciences, Sam Higginbottom Institute of Agriculture Technology & Sciences, Allahabad, India. udaysingh98@gmail.com
authors.forename: U P
authors.initials: UP
authors.lastname: Singh
authors.forename: H R
authors.initials: HR
authors.lastname: Bhat
authors.forename: P
authors.initials: P
authors.lastname: Gahtori
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D019306:Artemisia / Q000187:drug effects / Q000254:growth & development; D001234:Aspergillus niger / Q000187:drug effects*; D002176:Candida albicans / Q000187:drug effects*; D041221:Candida glabrata / Q000187:drug effects*; D003455:Cryptococcus neoformans / Q000187:drug effects*; D004353:Drug Evaluation, Preclinical; D007814:Larva; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D008970:Molecular Weight; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry / Q000494:pharmacology*; D014227:Triazines / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000935:Antifungal Agents; D013844:Thiazoles; D014227:Triazines