Cross, R. Matthew published the artcileSynthesis, Antimalarial Activity, and Structure-Activity Relationship of 7-(2-Phenoxyethoxy)-4(1H)-quinolones, Computed Properties of 209919-30-2, the publication is Journal of Medicinal Chemistry (2011), 54(24), 8321-8327, database is CAplus and MEDLINE.
Me 6-butyl-2-methyl-4-oxo-7-(2-phenoxyethoxy)-1,4-dihydroquinoline-3-carboxylate (I, ICI 56,780) displayed causal prophylactic and blood schizonticidal activity (ED50 = 0.05 mg/kg) in rodent malaria models but produced rapid acquisition of parasitol. resistance in P. berghei infected mice. Herein we describe the synthesis of analogs of I with EC50 as low as 0.15 nM against multidrug resistant P. falciparum. Optimal activity with low cross-resistance indexes (RI) to atovaquone was achieved by introducing ortho-substituted aryl moieties at the 3-position of the 7-(2-phenoxyethoxy)-4(1H)-quinolone core.
Journal of Medicinal Chemistry published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Computed Properties of 209919-30-2.
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