Calas, Michele; Ouattara, Mahama; Piquet, Gilles; Ziora, Zyta; Bordat, Y.; Ancelin, Marie L.; Escale, Roger; Vial, Henri published the artcile< Potent Antimalarial Activity of 2-Aminopyridinium Salts, Amidines, and Guanidines>, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine, the main research area is aminopyridinium salt amidine guanidine derivative preparation antimalarial malaria Plasmodium.
The authors describe the design, synthesis, and antimalarial activity of 60 bis-tertiary amine, bis-2(1H)-imino-heterocycle, bis-amidine, and bis-guanidine series. Bis-tertiary amines with a linker from 12 to 16 methylene groups were active against the in vitro growth of Plasmodium falciparum within the 10-6-10-7 M concentration range. IC50 decreased by 2 orders of magnitude for bis-2-aminopyridinium salts, bis-amidines, and bis-guanidines (27 compounds with IC50 < 10 nM). Increasing the alkyl chain length from 6 to 12 methylene groups led to increased activity, while beyond this antimalarial activity decreased. Antimalarial activities appear to be strictly related to the basicity of the cationic head with an optimal pKa over 12.5. Maximal activity occurs for bis-2-aminopyridinium, two C-duplicated bis-amidines, and three bis-guanidines, with IC50 values lower than 1 nM. In comparison to similar quaternary ammonium salts, amidinium compounds have distinct structural requirements for antimalarial activity and likely addnl. binding opportunities on account of their hydrogen-bond-forming properties. Journal of Medicinal Chemistry published new progress about Antimalarials. 70057-67-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H6ClN3S, Recommanded Product: 5-(3-Chlorophenyl)-1,3,4-thiadiazol-2-amine.
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