European Journal of Medicinal Chemistry p. 735 - 745 (2018)
Update date:2022-08-04
Topics:
Yadav, Neesha
Agarwal, Drishti
Kumar, Satyanand
Dixit
Gupta, Rinkoo D.
Awasthi, Satish K.
Twenty two diverse coumarin-triazole derivatives were synthesized by alkylation of 7-hydroxy-4-methyl-coumarin followed by click chemistry at 7-position. These compounds were evaluated for their in vitro antiplasmodial activity against chloroquine sensitive strain of Plasmodium falciparum (3D7). Compound 9 (7-[1-(2, 4-dimethoxy-phenyl)-1H- [1–3] triazol-4-ylmethoxy]-4-methyl-chromen-2-one) was found most active with IC50 value 0.763 ± 0.0124 μg/mL. Further, the structure of compound 20 was characterized by single crystal X-ray diffraction. In view of impressive results, we considered it worthwhile to validate the results of in vitro antiplasmodial activity by assessing whether these compounds are capable of hampering the catalytic activity of DNA gyrase, thus preventing its supercoiling function.
View MoreSHAANXI TOP PHARM CHEMICAL CO.LTD
Contact:+86-029-85733403
Address:No.108 ,west sector,south er huan,xi'an,china
Tianjin Ingenochem Technology Co.,Ltd
Contact:+86-22-23677060
Address:Hitech Green Industry Park K2-9-602, Nankai district
China Synchem Technology Co.,Ltd
website:http://www.cnsynchem.com
Contact:+86-0552-4929311
Address:No.217 Daqing Road
Huangshan Honghui Pharm Technology Co., Ltd.(expird)
website:http://www.honghuichem.com
Contact:18855958372
Address:Qingshan Wan No.1,Nanyuan Kou,SheXian Huangshan City,Anhui Province
Nanjing Raise Pharmatech Co., Ltd
website:http://www.raisechem.com
Contact:+86-25-58649566
Address:B381,No.606,Ningliu Road,Jiangbei New Area,Nanjing,Jiangsu Province,China
Doi:10.1039/jr9550000374
(1955)Doi:10.1021/jm001134q
(2001)Doi:10.1016/j.tetlet.2007.07.175
(2007)Doi:10.1021/acs.jmedchem.9b01658
(2020)Doi:10.1021/acscatal.1c01840
(2021)Doi:10.1002/hlca.19720550302
(1972)