Antimalarial quinolones: synthesis, potency, and mechanistic studies
RW Winter, JX Kelly, MJ Smilkstein, R Dodean… - Experimental …, 2008 - Elsevier
In the present article we examine the antiplasmodial activities of novel quinolone derivatives
bearing extended alkyl or alkoxy side chains terminated by a trifluoromethyl group. In the
series under investigation, the IC50 values ranged from 1.2 to≈ 30nM against chloroquine-
sensitive and multidrug-resistant Plasmodium falciparum strains. Modest to significant cross-
resistance was noted in evaluation of these haloalkyl-and haloalkoxyquinolones for activity
against the atovaquone-resistant clinical isolate Tm90-C2B, indicating that a primary target …
bearing extended alkyl or alkoxy side chains terminated by a trifluoromethyl group. In the
series under investigation, the IC50 values ranged from 1.2 to≈ 30nM against chloroquine-
sensitive and multidrug-resistant Plasmodium falciparum strains. Modest to significant cross-
resistance was noted in evaluation of these haloalkyl-and haloalkoxyquinolones for activity
against the atovaquone-resistant clinical isolate Tm90-C2B, indicating that a primary target …
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