International Journal of Biological Macromolecules p. 1096 - 1106 (2017)
Update date:2022-08-11
Topics:
Liu, Jing
Li, Mengrong
Yu, Yanying
Cao, Shuwen
Novel Tyrosinase Inhibitors of 4-functionalized Thiophene-2-carbaldehyde thiosemicarbazone (TCT) derivatives (1–8) had been synthesized and Spectrofluorimetry, 1H and 13C NMR titration and Molecular docking had been used to investigate their inhibitory activities and mechanisms on tyrosinase. The results showed that the inter-molecular interactions or hydrogen bond formation by increasing length of carbon chain or introducing benzene ring to the 4-functionalized ester group promoted or stabilized formation of complexes between modifier and tyrosinase, and enhanced the inhibitory activity of modifiers. The inhibitory activity of 4-benzoy methoxy-TCT was much stronger than that of any other synthesized tested modifiers, which was well explained by molecular docking and further verified by spectrofluorimetry and NMR titration by assuming that there existed an inter-molecular interaction besides formation of hydrogen bonds between the amino acid residues ASN260, GLU256, HIS85 of enzyme and the modifier.We concluded that 4-benzoy methoxy substitution of TCT was a good route obtaining novel tyrosinase inhibitors and deserved further studies.
View Morewebsite:http://www.fwdchem.com
Contact:86-21-54450828
Address:Room 802,Lotus Tower ,159 Tianzhou Road,Xuhui District,Shanghai
Yurui(Shanghai)Chemical Co.,Ltd
Contact:0086 21-50456736
Address:No.3188 Xiupu Road,Shanghai
shijiazhuang alkay chemicals co..ltd
Contact:86-311-67692035
Address:2601,juntang building,qiaodong district,shijiazhuang
TAIXING BEST NEW MATERIALS CO., LTD
Contact:0523-87998158;
Address:No.18 Zhonggang Road,Taixing City ,Jiangsu , China
TIANJIN NORTH JINHENG CHEMICAL PLANT.
Contact:0086-22-59952083
Address:DongShigu Country In JiXian TianJin China
Doi:10.1039/P29790001653
(1979)Doi:10.1007/s11178-005-0047-8
(2004)Doi:10.1002/ardp.19763090612
(1976)Doi:10.1002/chem.202100043
(2021)Doi:10.1021/jp980215j
(1998)Doi:10.1097/00005537-200205000-00020
(1906)