title: Synthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity.
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 IC500.037, 0.044 and 0.042 μM, respectively, while IC50of thiourea is 20.9 μM.
authors: a Department of Physico-Chemical Hazards of Health and Ecology , Institute of Rural Health , Lublin , Poland.|b Department of Chemistry , Siedlce University of Natural Sciences and Humanities , Siedlce , Poland.
authors: Mariusz
authors: M
authors: Mojzych
authors: a Department of Physico-Chemical Hazards of Health and Ecology , Institute of Rural Health , Lublin , Poland.
authors: Paweł
authors: P
authors: Tarasiuk
authors: c Department of Hematooncology and Bone Marrow Transplantation Unit , Medical University of Lublin , Lublin , Poland.
authors: Katarzyna
authors: K
authors: Kotwica-Mojzych
authors: d Department of Biology , Kongju National University , Gongju , Republic of Korea.|e Department of Biochemistry and Biotechnology (Baghdad-ul-Jadeed Campus) , The Islamia University of Bahawalpur , Pakistan.
authors: Muhammad
authors: M
authors: Rafiq
authors: d Department of Biology , Kongju National University , Gongju , Republic of Korea.
authors: Sung-Yum
authors: SY
authors: Seo
authors: b Department of Chemistry , Siedlce University of Natural Sciences and Humanities , Siedlce , Poland.
authors: Michał
authors: M
authors: Nicewicz
authors: f EMF Lab , Lublin , Poland.
authors: Emilia
authors: E
authors: Fornal
mesh_terms: D066241:Carbon-13 Magnetic Resonance Spectroscopy; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors*; D066244:Proton Magnetic Resonance Spectroscopy; D011720:Pyrazoles / Q000737:chemistry*; D013237:Stereoisomerism; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology*; D014227:Triazines / Q000737:chemistry*; D014510:Urease / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; D011720:Pyrazoles; D013449:Sulfonamides; D014227:Triazines; D014442:Monophenol Monooxygenase; D014510:Urease
keywords: Pyrazolo[4,3-e][1,2,4]triazine; sulfonamides; tyrosinase inhibitors; urease inhibitors