Molecules (2017)
Update date:2022-08-03
Topics:
Peperidou, Aikaterini
Pontiki, Eleni
Hadjipavlou-Litina, Dimitra
Voulgari, Efstathia
Avgoustakis, Konstantinos
Our research to discover potential new multitarget agents led to the synthesis of 10 novel derivatives of cinnamic acids and propranolol, atenolol, 1-adamantanol, naphth-1-ol, and (benzylamino) ethan-1-ol. The synthesized molecules were evaluated as trypsin, lipoxygenase and lipid peroxidation inhibitors and for their cytotoxicity. Compound 2b derived from phenoxyphenyl cinnamic acid and propranolol showed the highest lipoxygenase (LOX) inhibition (IC50 = 6 uM) and antiproteolytic activity (IC50 = 0.425 uM). The conjugate 1a of simple cinnamic acid with propranolol showed the higher antiproteolytic activity (IC50 = 0.315 uM) and good LOX inhibitory activity (IC50 = 66 uM). Compounds 3a and 3b, derived from methoxylated caffeic acid present a promising combination of in vitro inhibitory and antioxidative activities. The S isomer of 2b also presented an interesting multitarget biological profile in vitro. Molecular docking studies point to the fact that the theoretical results for LOX-inhibitor binding are identical to those from preliminary in vitro study.
View MoreYangzhou Zhongbao Pharmaceutical Co.,Ltd
Contact:+86-514-88290838
Address:Jiangsu Baoying county economic develpment zone in baoying avenue91
taicang liyuan chemical co,.ltd
website:http://www.tcliyuanchem.com/productse.php
Contact:86-512-53539583
Address:Room 804,Huaxu Building,No.95,Renmin South Road,Taicang city,Jiangsu Province,China
jiangsu hualin chemical co.,ltd.
Contact:86-25-87787402
Address:jaingsu,china
Shanghai Xinda Pharmaceuticals Co., Ltd.
Contact:86-21-33692333-8008
Address:999 Linxian Road, Jinshan Industrial Park, Shanghai, China
Guilin Zhenda Bio-Tech Co., Ltd.
Contact:86-773-3568977
Address:-Yangtang shangshui industry park, Lingui county,
Doi:10.1002/anie.201206305
(2013)Doi:10.1016/0039-128X(86)90020-6
(1986)Doi:10.1039/j39710000074
(1971)Doi:10.1016/S0040-4039(00)81858-4
(1983)Doi:10.1248/cpb.54.458
(2006)Doi:10.1002/hlca.19800630422
(1980)