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Azabenzimidazoles are among the substrates most frequently found in small-molecule drugs due to their broad-spectrum biological activity. Newer drugs are continually in need of to replace existing drugs which encounter microorganism drug resistance. The reaction of 2,3-diaminopyridine precursors with variously substituted benzaldehydes has provided convenient and efficient access to a series of 4-azabenzimidazole derivatives and, regioselectively, to a series of 2-amino-5-bromo-3-(phenylimino)pyridine derivatives, while sodium cyanoborohydride reduction of the latter has afforded the corresponding 2-amino-5-bromo-3- (phenylamino)pyridine analogues. Bioassays of these and other compounds have been undertaken to explore their cytotoxicity and their activity against the parasitic protozoans, Plasmodium falciparum and Trypanosoma brucei. A number of the compounds show promising selective activity against T. brucei with IC50 values as low as 1.3 µM while two of them exhibit encouraging activity against both T. brucei and P. falciparum. [ABSTRACT FROM AUTHOR]

A small library of nine, novel 2,4-diarylquinoline derivatives has been prepared in high yield via convenient one- or two-step routes from a series of substituted 2-aminobenzophenones. None of the products exhibited toxicity at 20 μM against human cervix adenocarcinoma (HeLa) cells, while many of them exhibited encouraging trypanocidal activity against T. brucei brucei (a parasite responsible for African cattle trypanosomiasis) - some with IC50 values in the range 2.8 - 6.2 μM. [ABSTRACT FROM AUTHOR]