NOVEL INDOLYLQUINOLINE-PHENYLAMIDINE COMPOUNDS AS ANTILEISHMANIAL AGENTS AND THE PROCESS OF PREPARATION THEREOF

摘要

The present invention relates to novel indolylquinoline-phenylamidines of formula I and the process of preparation thereof. The synthesized indolylquinoline-phenylamidines were tested for their antileishmanial activity in which the compounds showed activity as potent antileishmanial agents. The compounds show more activity and lesser toxicity than Pentamindine, a known antileishmanial drug, which is used as positive standard. Compound C1 (SKG-9-5) and C2 (SKG-9-6) were found to be most potent with IC50 value, 5 �M for both, while Pentamidine showed IC50 7.5 �M. The compounds were found less toxic to normal cells compared to Pentamidine. Very interestingly, the cytotoxicity to normal cell is about 40 times less in comparison to promastigote-IC50 value.