Synthesis and evaluation of new diaryl ether and quinoline hybrids as potential antiplasmodial and antimicrobial agents
Synthesis and bioevaluation of new diaryl ether hybridized quinoline derivatives as antiplasmodial, antibacterial and antifungal agents is reported. It was encouraging to discover that several compounds displayed 2-3 folds better efficacy than chloroquine in chloroquine-resistant K1 strain of Plasmodium falciparum. Further, a few members of the library displayed good antibacterial efficacy against gram positive strains of bacteria but none of the compounds displayed any significant antifungal activity.
The invention relates to heterocyclic derivatives, to the use of said derivatives in treating a range of metabolic diseases and other conditions mediated by agonism of the G-protein coupled bile acid GPBAR1/TGR5 receptor, to compositions and formulations containing said derivatives, processes for their preparation and methods of delivery.
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(2015/01/09)
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