Synthesis of pyrazolo[4,3-e][1,2,4]triazine sulfonamides, novel Sildenafil analogs with tyrosinase inhibitory activity

被引：28

作者：

Mojzych, Mariusz ^{[1
]}

Dolashki, Aleksandar ^{[2
]}

Voelter, Wolfgang ^{[3
]}

机构：

[1] Siedlce Univ Nat Sci & Humanities, Dept Chem, PL-08110 Siedlce, Poland

[2] Bulgarian Acad Sci, Ctr Phytochem, Inst Organ Chem, BU-1113 Sofia, Bulgaria

[3] Interfacultary Inst Biochem, D-72076 Tubingen, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2014年 / 22卷 / 23期

关键词：

Denovo synthesis; Inhibitors; aza-Sildenafil; aza-isoViagra; ORGANIC-SYNTHESIS; CYCLOCONDENSATION; 1,2,4-TRIAZINES; ETHER;

D O I：

10.1016/j.bmc.2014.10.009

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Tyrosinase is a multifunctional, glycosylated and copper-containing oxidase which catalyzes the first two steps in mammalian melanogenesis and is responsible for enzymatic browning reactions in damaged fruits during post-harvest handling and processing. Neither hyperpigmentation in human skin nor enzymatic browning in fruits are desirable. These phenomena have encouraged researchers to seek new potent tyrosinase inhibitors for use in foods and cosmetics. This article surveys tyrosinase inhibitors, newly discovered from natural and synthetic sources. The inhibitory strength is comparable to that of the standard inhibitor kojic acid. Also their inhibitory mechanisms are discussed. The new obtained compounds were also tested as PDE5 inhibitors and did not show significant inhibitory effect. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：6616 / 6624

页数：9

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