NOVEL CLASS OF HYBRID NATURAL PRODUCTS DERIVED FROM LUPEOL (PART-III) PHARMACOMODULATION ON LUPEOL SKELETON : DESIGN, SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL LUPEOL DERIVATIVES AS ANTIMALARIAL AGENTS

摘要

Novel hybrid lupeol heterocyclics (quinoline, pyrimidine and pyrazole) were prepared. Triterpene lupeol 1 isolated from plant Crataeva nurvala was chemically modified and hybrid natural products 2a, 3a-p, 4a-p, 5a-b, 6e, 7a-b, 8a-c, 9 and 10 were evaluated for antimalarial activity in vitro. Compounds 3g, 3e, 3i, 4e, 4f, 5e, 7b and 8c showed MIC against chloroquine sensitive 3D7 strain of P. falciparum at 10 mu g/ml.