Pyridinium azolate betaines and their derivatives: A new class of antiprotozoal agents

Article abstract of DOI:10.1016/0223-5234(90)90114-I

N-azolylpyridinium salts 1 and several betaines of pyridinium azolate 2 have been synthesized in order to study their in vitro antiprotozoal activity. A careful ¹H and ¹³C-NMR study has been carried out in order to characterize the different compounds. A significant growth inhibition of Trypanosoma cruzi and especially Leishmania donovani was observed with the N-benzimidazolylpyridinium derivatives. When tested in vivo against Leishmania donovani, compounds 9 and 40 have had a much greater reducing effect in the parasite than that of the reference drug (glucantime).