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J Enzyme Inhib Med Chem. 2017 Dec;32(1):99-105. doi: 10.1080/14756366.2016.1238362. Epub 2016 Oct 25.

Synthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity.

Author information

1
a Department of Physico-Chemical Hazards of Health and Ecology , Institute of Rural Health , Lublin , Poland.
2
b Department of Chemistry , Siedlce University of Natural Sciences and Humanities , Siedlce , Poland.
3
c Department of Hematooncology and Bone Marrow Transplantation Unit , Medical University of Lublin , Lublin , Poland.
4
d Department of Biology , Kongju National University , Gongju , Republic of Korea.
5
e Department of Biochemistry and Biotechnology (Baghdad-ul-Jadeed Campus) , The Islamia University of Bahawalpur , Pakistan.
6
f EMF Lab , Lublin , Poland.

Abstract

A new series of sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazine with chiral amino group has been synthesized and characterized. The compounds were tested for their tyrosinase and urease inhibitory activity. Evaluation of prepared derivatives demonstrated that compounds (8b) and (8j) are most potent mushroom tyrosinase inhibitors whereas all of the obtained compounds showed higher urease inhibitory activity than the standard thiourea. The compounds (8a), (8f) and (8i) exhibited excellent enzyme inhibitory activity with IC50 0.037, 0.044 and 0.042 μM, respectively, while IC50 of thiourea is 20.9 μM.

KEYWORDS:

Pyrazolo[4,3-e][1,2,4]triazine; sulfonamides; tyrosinase inhibitors; urease inhibitors

PMID:
27778522
PMCID:
PMC6010123
DOI:
10.1080/14756366.2016.1238362
[Indexed for MEDLINE]
Free PMC Article

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