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

Autor:	Mariusz Mojzych, Paweł Tarasiuk, Katarzyna Kotwica-Mojzych, Muhammad Rafiq, Sung-Yum Seo, Michał Nicewicz, Emilia Fornal
Jazyk:	angličtina
Rok vydání:	2017
Předmět:	Pyrazolo[4 3-e][1 2 4]triazine sulfonamides tyrosinase inhibitors urease inhibitors Therapeutics. Pharmacology RM1-950
Zdroj:	Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 32, Iss 1, Pp 99-105 (2017)
Druh dokumentu:	article
ISSN:	1475-6366 1475-6374 14756366
DOI:	10.1080/14756366.2016.1238362
Popis:	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.
Databáze:	Directory of Open Access Journals
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