Abstract
AbstractA series of quinoline derivatives containing a 2‐thienyl ring in the 2‐position and CO2H, CH2OH, CHO, CH(OH)CN, CH(OH)CO2H, CO2C2H5, COCH[N(C2H5)2]CO2C2H5, COCH2N(C2H5)2, COCH3, magnified image substituents in the 4‐position was synthesized. Both intermediate and target compounds were tested for antimalarial activity. A second series with a 5‐bromo‐2‐thienyl group in the 2‐position and CHOHCH2N(C2H5)2, CHOHCH2N(CH2)6, and CHOHCH2N(CH2C6H5)2 substituents in the 4‐position was also prepared, it was found that, although these quinoline methanols were moderately active antimalarials, they exhibited a high degree of phototoxicity. A third series of compounds with 2‐alkyl substituents (methyl, t‐butyl) was also synthesized, and these were found to combine a modest degree of antimalarial activity with low phototoxicity. Several novel synthetic routes to the above compounds were developed and are detailed.
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