Structure-activity relationships and mechanistic studies of novel mitochondria-targeted, leishmanicidal derivatives of the 4-aminostyrylquinoline scaffold
作者:Matteo Staderini、Marta Piquero、María Ángeles Abengózar、Montserrat Nachér-Vázquez、Giulia Romanelli、Pilar López-Alvarado、Luis Rivas、Maria Laura Bolognesi、J. Carlos Menéndez
DOI:10.1016/j.ejmech.2019.03.007
日期:2019.6
A new class of quinoline derivatives, bearing amino chains at C-4 and a styryl group at C-2, were tested on Leishmania donovani promastigotes and axenic and intracellular Leishmania pifanoi amastigotes. The introduction of the C-4 substituent improves the activity, which is due to interference with the mitochondrial activity of the parasite and its concomitant bioenergetic collapse by ATP exhaustion
N-type calcium channel antagonists for the treatment of pain
申请人:——
公开号:US20040053964A1
公开(公告)日:2004-03-18
Compounds useful for the treatment of pain in accord with the following structural diagram,
1
wherein R
1
, R
2
, R
3
, R
4
and R
5
are any of a number of groups as defined in the specification, A and D are as defined in the specification, and pharmaceutical compositions and methods of treatment utilising such compounds.