Molecules p. 43 - 51 (2015)
Update date:2022-09-26
Topics:
Menezes, Jlio Csar L.
Vaz, Luana Beatriz A.
De Vieira, Paula Melo Abreu
Fonseca, Ktia Da Silva
Carneiro, Cludia Martins
Taylor, Jason G.
Chagas disease is a so-called "neglected disease" and endemic to Latin America. Nifurtimox and benznidazole are drugs that have considerable efficacy in the treatment of the acute phase of the disease but cause many significant side effects. Furthermore, in the Chronic Phase its efficiency is reduced and their therapeutic effectiveness is dependent on the type of T. cruzi strain. For this reason, the present work aims to drive basic research towards the discovery of new chemical entities to treat Chagas disease. Differently substituted 5,7-diaryl-2,3-dihydro-1,4-diazepines were synthesized by cyclocondensation of substituted flavones with ethylenediamine and tested as anti-Trypanosoma cruzi candidates. Epimastigotes of the Y strain from T. cruzi were used in this study and the number of parasites was determined in a Neubauer chamber. The most potent diaryldiazepine that reduced epimastigote proliferation exhibited an IC50 value of 0.25 μM, which is significantly more active than benznidazole.
View MoreNantong Kaixin Pharma Chemical Co.,Ltd.
Contact:86-513-85250786
Address:2-1103 Huachen Mansion, 111 Gongnong Road,Nantong, Jiangsu, China
Chengdu Baishixing Science and Technology Industry Co., Ltd.
website:http://www.cd-bsx.com
Contact:+86-28-88531548
Address:#217,North of Industry Road,Heshan Town,Pujiang County,Chengdu,Sichuan,China.
Yurui(Shanghai)Chemical Co.,Ltd
Contact:0086 21-50456736
Address:No.3188 Xiupu Road,Shanghai
Puyang Huicheng Electronic Material Co., Ltd
website:http://huichengchem.weba.testwebsite.cn/index_en.html
Contact:+86-393-8910800
Address:West Section Shengli Road, Puyang457000, China
Contact:0550-7041128 0550-7090578
Address:Wangdian Street,Xinjie Town
Doi:10.1021/jo00384a040
(1987)Doi:10.1246/bcsj.59.1031
(1986)Doi:10.1021/np010599w
(2002)Doi:10.1055/s-1986-31631
(1986)Doi:10.1016/j.bmcl.2008.07.029
(2008)Doi:10.1021/ja01598a057
(1956)