Leishmania donovani, Plasmodium berghei, Trypanosoma rhodesiense: Antiprotozoal effects of some amidine types

New Bis(2-aminoimidazoline) and Bisguanidine DNA Minor Groove Binders with Potent in Vivo Antitrypanosomal and Antiplasmodial Activity

“…Besides, the ip administration of 3b (30 mg/kg) produced an activity of 44.1% similar to its diamidine counterpart administered subcutaneously at 40 mg/kg. 31 Altogether, the data confirm the antimalarial potential of the diphenyl amine, diphenylether and diphenyl sulfide scaffolds.…”

Dicationic DNA Minor Groove Binders as Antimicrobial Agents

“…[14,15], Candida albicans [11-13, 16, 17], Cryptococcus neoformans [11][12][13], Cryptosporidium parvum [18,19], Giardia lamblia [20], Leishmania sp. [21][22][23][24][25], Mycobacterium tuberculosis [16], Plasmodium sp. [21,23,26], Pneumocystis carinii [27][28][29][30], Toxoplasma gondii [31], and Trypanosoma sp.…”

“…[21][22][23][24][25], Mycobacterium tuberculosis [16], Plasmodium sp. [21,23,26], Pneumocystis carinii [27][28][29][30], Toxoplasma gondii [31], and Trypanosoma sp. [32][33][34][35][36][37].…”

In situ potentiometric method to evaluate bacterial outer membrane-permeabilizing ability of drugs: Example using antiprotozoal diamidines

“…Diminazene and pentamidine have a long history as valuable chemotherapeutic agents against protozoan infections (Baraldi et al, 2004;Delespaux and De Koning, 2007;Steck et al, 1981). DAPI is also 2) at 2×10 9 CFU/mL.…”

“…We chose antiprotozoal and chemopreventive diamidines, along with a general chemical reagent, possessing two amidino groups. The compounds tested included diminazene (Baraldi et al, 2004;Delespaux and De Koning, 2007;Steck et al, 1981), pentamidine (Baraldi et al, 2004;Delespaux and De Koning, 2007;Steck et al, 1981), 4′,6-diamidino-2-phenylindole (DAPI) (Delespaux and De Koning, 2007), S,S′-1,4-phenylene-bis(1,2-ethanediyl)bisisothiourea (1,4-PBIT) (Chen et al, 2004), and 1,4-(diamidino)benzene (1,4-DAB). The chemical structure of the agents is shown in Fig.…”