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

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 propose...

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Main Authors: S. V. Kholodnyak, K. P. Shabelnik, S. I. Kovalenko, G. O. Gernova, S. D. Trzhеtsinskiy
Format: Article
Language:English
Published: Zaporizhzhia State Medical and Pharmaceutical University 2015-08-01
Series:Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki
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Online Access:http://pharmed.zsmu.edu.ua/article/view/45122/43755
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author S. V. Kholodnyak
K. P. Shabelnik
S. I. Kovalenko
G. O. Gernova
S. D. Trzhеtsinskiy
author_facet S. V. Kholodnyak
K. P. Shabelnik
S. I. Kovalenko
G. O. Gernova
S. D. Trzhеtsinskiy
author_sort S. V. Kholodnyak
collection DOAJ
description 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».
format Article
id doaj-art-16bfa90c4e774b229d02486bc7f1941f
institution Kabale University
issn 2306-8094
2409-2932
language English
publishDate 2015-08-01
publisher Zaporizhzhia State Medical and Pharmaceutical University
record_format Article
series Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki
spelling doaj-art-16bfa90c4e774b229d02486bc7f1941f2025-08-20T03:33:02ZengZaporizhzhia State Medical and Pharmaceutical UniversityAktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki2306-80942409-29322015-08-01291610.14739/2409-2932.2015.2.45122Purposeful search of hypoglycemic agents among N-arylcarbamides and N-arylsulfamides of [2-(3-R-1Н-[1,2,4]triazole-5-yl)phenyl]aminesS. V. KholodnyakK. P. ShabelnikS. I. KovalenkoG. O. GernovaS. D. TrzhеtsinskiyAim. 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».http://pharmed.zsmu.edu.ua/article/view/45122/437552-(3-R-1Н-[1 2 4]triazole-5-yl)phenyl]amines1 2 4-triasoleArylamine Acetylases ArylsulfatesN-arylcarbamidesHypoglycemics
spellingShingle S. V. Kholodnyak
K. P. Shabelnik
S. I. Kovalenko
G. O. Gernova
S. D. Trzhеtsinskiy
Purposeful search of hypoglycemic agents among N-arylcarbamides and N-arylsulfamides of [2-(3-R-1Н-[1,2,4]triazole-5-yl)phenyl]amines
Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki
2-(3-R-1Н-[1 2 4]triazole-5-yl)phenyl]amines
1 2 4-triasole
Arylamine Acetylases Arylsulfates
N-arylcarbamides
Hypoglycemics
title Purposeful search of hypoglycemic agents among N-arylcarbamides and N-arylsulfamides of [2-(3-R-1Н-[1,2,4]triazole-5-yl)phenyl]amines
title_full Purposeful search of hypoglycemic agents among N-arylcarbamides and N-arylsulfamides of [2-(3-R-1Н-[1,2,4]triazole-5-yl)phenyl]amines
title_fullStr Purposeful search of hypoglycemic agents among N-arylcarbamides and N-arylsulfamides of [2-(3-R-1Н-[1,2,4]triazole-5-yl)phenyl]amines
title_full_unstemmed Purposeful search of hypoglycemic agents among N-arylcarbamides and N-arylsulfamides of [2-(3-R-1Н-[1,2,4]triazole-5-yl)phenyl]amines
title_short Purposeful search of hypoglycemic agents among N-arylcarbamides and N-arylsulfamides of [2-(3-R-1Н-[1,2,4]triazole-5-yl)phenyl]amines
title_sort purposeful search of hypoglycemic agents among n arylcarbamides and n arylsulfamides of 2 3 r 1н 1 2 4 triazole 5 yl phenyl amines
topic 2-(3-R-1Н-[1 2 4]triazole-5-yl)phenyl]amines
1 2 4-triasole
Arylamine Acetylases Arylsulfates
N-arylcarbamides
Hypoglycemics
url http://pharmed.zsmu.edu.ua/article/view/45122/43755
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