ChemMedChem p. 966 - 975 (2021)
Update date:2022-07-30
Topics:
Silva, Daniel G.
Junker, Anna
de Melo, Shaiani M. G.
Fumagalli, Fernando
Gillespie, J. Robert
Molasky, Nora
Buckner, Frederick S.
Matheeussen, An
Caljon, Guy
Maes, Louis
Emery, Flavio S.
Neglected tropical diseases remain among the most critical public health concerns in Africa and South America. The drug treatments for these diseases are limited, which invariably leads to fatal cases. Hence, there is an urgent need for new antitrypanosomal drugs. To address this issue, a large number of diverse heterocyclic compounds were prepared. Straightforward synthetic approaches tolerated pre-functionalized structures, giving rise to a structurally diverse set of analogs. We report on a set of 57 heterocyclic compounds with selective activity potential against kinetoplastid parasites. In general, 29 and 19 compounds of the total set could be defined as active against Trypanosoma cruzi and T. brucei brucei, respectively (antitrypanosomal activities <10 μM). The present work discusses the structure?activity relationships of new fused-ring scaffolds based on imidazopyridine/pyrimidine and furopyridine cores. This library of compounds shows significant potential for anti-trypanosomiases drug discovery.
View MoreTIANJIN GST CHEMICAL TECHNOLOGY CO., LTD
Contact:+86-22-25210964
Address:Room. 208, No. -12-C, No. 13, Xinbei Road, Tanggu District, New Haixin Area, Tianjin City, China
website:http://www.angchenchem.com
Contact:+86-510-88302099 82327577
Address:Rm. 404/405, Floor 4th, No. 983 FengXiang Road, Wuxi, China
TIANJIN ZHONGXIN CHEMTECH CO.,LTD.
Contact:86-022-89880739
Address:10B, Pan China International Center, No. 931 YingKou Road, TangGu, Tianjin, China, 300451
Shanghai Sunway Pharmaceutical Technology Co.,Ltd.
Contact:+86-21-5161 3915
Address:Shanghai YangPu
website:http://www.josunpharma.com
Contact:+86-311-80715268 80766839
Address:No.39, Zhaiying Street, Shijaizhuang,Hebei,China
Doi:10.1021/acscatal.6b00628
(2016)Doi:10.1021/ja01550a082
(1958)Doi:10.1016/j.tetasy.2009.07.038
(2009)Doi:10.1021/jo901913h
(2009)Doi:10.1155/2010/524124
(2010)Doi:10.1002/ejoc.200900669
(2009)