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A series of 4-alkylaminoaryl phenyl cyclopropyl methanones (
6a–
6u and
8a–
8c) were synthesized from 4-fluorochalcones (
3a and
3b) by cyclopropanation of double bond followed by nucleophilic substitution of F with different amines. The compounds were screened for their antitubercular and antimalarial activities against
Mycobacterium tuberculosis H37Rv and
Plasmodium falciparum 3D7 strains in vitro respectively. Several compounds (
6a,
6d–
6h,
6p,
6q and
8a–
8c) exhibited good in vitro antitubercular activities with MIC values 3.12–12.5
μg/mL and preferentially inhibited the growth of
P. falciparum in vitro (
4a,
4c,
6a–
6d,
6f,
6s,
8a and
8c) with IC
50 as low as 0.080 and 0.035
μg/mL and SI values 4975 and 6948, respectively. Molecular docking studies and in vitro evaluation against FAS-II enzymes using reporter gene assays were carried out to elucidate the mode of action of these molecules. Two compounds
4a and
6g showed significant inhibition at 25
μM concentration of the compound.