Synthesis, characterization and biological screening of some 3-phenyl indole derivatives

Abstract

In an attempt to search for new and alternative antimalarial agents, a series of 2-(4-amino sulfonyl phenyl) 3-phenyl indole substituted amine derivative -2-(4-amino sulfonyl phenyl) 3-phenyl-5 chloro indole and 2-(4-amino sulfonyl phenyl) 3-phenyl -5 fluoro indole derivatives were synthesized and their chemical structures confirmed by Elemental, 1H NMR, IR and mass spectrophotometric analysis. The in vitro antimalarial activities of these compounds were evaluated against the chloroquine-sensitive (D10) and the chloroquine-resistant (RSA11) strains of Plasmodium falciparum. The 2-(4-amino sulfonyl phenyl) 3-phenyl -5 chloro indole derivatives increased in vitro activity when compared to the unsubstituted analogues, which are all devoid of activity. The presence of the 5- chloro, fluoro, amine, mehoxy, hydroxy group in the indole ring system leads to compounds with diminished anti malarial activity when compared to the corresponding unsubstituted analogues. The compounds associate with ferriprotoporphyrin.