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Water soluble biguanide salts and their 1,3,5-triazine derivatives as inhibitors of acetylcholinesterase and α-glucosidase

Water soluble biguanide salts and their 1,3,5-triazine derivatives as inhibitors of... AbstractSeven biguanide derivatives were prepared by the nucleophilic reaction between dicyandiamide and p-substitute aniline derivatives or memantine or adamantine under acidic conditions. The cyclization of the biguanide compounds were also conducted via acetone to give 1,3,5-triazine derivatives. The structures of the synthesized compounds were characterized by analytical methods. The solid state structures of [HL5]Cl, [H2L7]Cl2, [HL1a]Cl and [HL5a]Cl were investigated by X-ray diffraction study. The acetylcholinesterase and α-glucosidase inhibitor properties of the compounds were then evaluated by the spectroscopic method. The compounds were found to show considerable acetylcholinesterase and α-glucosidase inhibitory activities compared to the approved drugs. The cyclization of biguanide derivatives with acetone did not affect inhibition of acetylcholinesterase, yet increased the α-glucosidase inhibition. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Zeitschrift für Kristallographie - Crystalline Materials de Gruyter

Water soluble biguanide salts and their 1,3,5-triazine derivatives as inhibitors of acetylcholinesterase and α-glucosidase

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Publisher
de Gruyter
Copyright
© 2020 Walter de Gruyter GmbH, Berlin/Boston
ISSN
2196-7105
eISSN
2196-7105
DOI
10.1515/zkri-2020-0025
Publisher site
See Article on Publisher Site

Abstract

AbstractSeven biguanide derivatives were prepared by the nucleophilic reaction between dicyandiamide and p-substitute aniline derivatives or memantine or adamantine under acidic conditions. The cyclization of the biguanide compounds were also conducted via acetone to give 1,3,5-triazine derivatives. The structures of the synthesized compounds were characterized by analytical methods. The solid state structures of [HL5]Cl, [H2L7]Cl2, [HL1a]Cl and [HL5a]Cl were investigated by X-ray diffraction study. The acetylcholinesterase and α-glucosidase inhibitor properties of the compounds were then evaluated by the spectroscopic method. The compounds were found to show considerable acetylcholinesterase and α-glucosidase inhibitory activities compared to the approved drugs. The cyclization of biguanide derivatives with acetone did not affect inhibition of acetylcholinesterase, yet increased the α-glucosidase inhibition.

Journal

Zeitschrift für Kristallographie - Crystalline Materialsde Gruyter

Published: Oct 25, 2020

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