Potential Antimalarials. XIX. Syntheses and Testing of α-(Piperidin-2-yl)-α-(7′-trifluoromethylquinolin-4′-yl)methanol and α-(7-Bromo-1,5-naphthyridin-4-yl)-α-(piperidin-2′-yl)methanol

التفاصيل البيبلوغرافية
العنوان: Potential Antimalarials. XIX. Syntheses and Testing of α-(Piperidin-2-yl)-α-(7′-trifluoromethylquinolin-4′-yl)methanol and α-(7-Bromo-1,5-naphthyridin-4-yl)-α-(piperidin-2′-yl)methanol
المؤلفون: Barlin, GB, Ireland, SJ, Jiravinyu, C, Nguyen, TMT, Kotecka, B, Rieckmann, KH
المصدر: Australian Journal of Chemistry; 1993, Vol. 46 Issue: 11 p1695-1703, 9p
مستخلص: The synthesis of the mefloquine analogue α-(piperidin-2-yl)-α-(7′-trifluoromethylquinolin-4′-yl)methanol (1) from 4-bromo-7-trifluoromethylquinoline and N-(hex-5-enyl) phthalimide through N-{4-[3′-(7″-trifluoromethylquinolin-4″-yl)oxiran-2′-yl]butyl} phthalimide 1′-oxide is reported. α-(7-Bromo-1,5-naphthyridin-4-yl)-α-(piperidin-2′-yl)methanol (2) was prepared by similar procedures. In tests against the K-1 isolate of Plasmodium falciparum, compound (1) proved the more active (IC50 99 nM ).
قاعدة البيانات: Supplemental Index
الوصف
تدمد:00049425
14450038
DOI:10.1071/CH9931695