399040-49-4Relevant academic research and scientific papers
Synthesis of quinolinyl chalcones and evaluation of their antimalarial activity
Dominguez, Jose N,Charris, Jaime E,Lobo, Gricela,Gamboa De Dominguez, Neira,Moreno, Maria M,Riggione, Flavia,Sanchez, Erlinda,Olson, Jed,Rosenthal, Philip J
, p. 555 - 560 (2001)
Quinolinyl chalcones were synthesized and evaluated for their inhibition of the Plasmodium falciparum cystein protease falcipain and their activity against cultured P. falciparum parasites. They were also tested for in vivo efficacy in a rodent P. berghei model. Their activity against falcipain and as antimalarials was moderate, but antimalarial activity was probably not due to the inhibition of falcipain and may follow a different mechanism. 1-(2,4-Dichlorophenyl)-3-[3-(2-chloro-6,7-dimethoxiquinolinyl)]-2-propen-1- one 3j was the most promising compound among those here reported (IC50 19.0 μM).
In vitro antifungal evaluation and structure-activity relationships of a new series of chalcone derivatives and synthetic analogues, with inhibitory properties against polymers of the fungal cell wall
Lopez, Silvia N.,Castelli, Maria V.,Zacchino, Susana A.,Dominguez, Jose N.,Lobo, Gricela,Charris-Charris, Jaime,Cortes, Juan C.G.,Ribas, Juan C.,Devia, Cristina,Rodriguez, Ana M.,Enriz, Ricardo D.
, p. 1999 - 2013 (2007/10/03)
Here we report the synthesis, in vitro antifungal evaluation and SAR study of 41 chalcones and analogues. In addition, all active structures were tested for their capacity of inhibiting Saccharomyces cerevisiae β(1,3)-glucan synthase and chitin synthase,
