Purposeful search of hypoglycemic agents among N-arylcarbamides and N-arylsulfamides of [2-(3-R-1Н-[1,2,4]triazole-5-yl)phenyl]amines

Authors

  • S. V. Kholodnyak
  • K. P. Shabelnik
  • S. I. Kovalenko
  • G. O. Gernova
  • S. D. Trzhеtsinskiy

DOI:

https://doi.org/10.14739/2409-2932.2015.2.45122

Keywords:

2-(3-R-1Н-[1, 2, 4]triazole-5-yl)phenyl]amines, 1, 4-triasole, Arylamine Acetylases Arylsulfates, N-arylcarbamides, N-arylsulfamides, Hypoglycemics

Abstract

Aim. Formation of N-arylcarbamides and N-arylsulfamides as result of interaction of 2-(3-R-1Н-[1,2,4]triazole-5-yl)phenyl]amines with electrophilic reagents (arylisocyanates and arylsulfonylchlorides) is described in presented article. The optimal conditions for mentioned reactions have been proposed.

Methods and results. It has been evaluated that N-arylcarbamides of 2-(3-aryl-1H-1,2,4-triazole-5-yl)phenyl]amines while heating over 90°C in glacial acetic acid undergo cyclisation followed by formation of corresponding 2-aryl-[1,2,4]triazolo[1,5-c]quinazoline-5(6Н)-ones. Purity and structure of synthesized compounds has been proved by elemental analysis, 1H NMR-, chromato-mass and mass-spectra.

Conclusion. It has been established, that compound 2.1 during evaluation of specific pharmacologic activities on oral glucose tolerance test (OGTT), rapid insulin and adrenaline test models exhibited action which is comparable to activities of reference-drugs «Metformin» and «Gliclazide».

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How to Cite

1.
Kholodnyak SV, Shabelnik KP, Kovalenko SI, Gernova GO, Trzhеtsinskiy SD. Purposeful search of hypoglycemic agents among N-arylcarbamides and N-arylsulfamides of [2-(3-R-1Н-[1,2,4]triazole-5-yl)phenyl]amines. Current issues in pharmacy and medicine: science and practice [Internet]. 2015Jul.14 [cited 2024Nov.13];(2). Available from: http://pharmed.zsmu.edu.ua/article/view/45122

Issue

No. 2 (2015)

Section

Synthesis of the biologically active compounds

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