Liu, Zong-ying published the artcileSynthesis and antiparasitic activity of new bis-arylimidamides: DB766 analogs modified in the terminal groups, Computed Properties of 4604-72-2, the publication is European Journal of Medicinal Chemistry (2014), 167-173, database is CAplus and MEDLINE.
Fifteen novel bis-arylimidamide derivatives with various 6-membered and 5-membered heterocyclic rings replacing the terminal pyridyl rings of the lead compound DB766, were prepared and evaluated vs. Trypanosoma cruzi, Leishmania amazonensis, Trypanosoma brucei rhodesiense and Plasmodium falciparum. Compound I(R = 2-pyrimidyl) with pyrimidine replacing the pyridine rings showed good activity vs. T. cruzi, T. brucei rhodesiense and P. falciparum (IC50 = 200 nM, 32 nM and 8.5 nM, resp.). Three compounds I(R = 2-methyl-4-thiozolyl, 2-methylamino-4-thiozolyl, 2-acetylamino-4-thiozolyl) with thiazole replacing the pyridine rings gave low micromolar (0.17-0.3 μM) IC50 values vs. L. amazonensis, however only 7g exhibited an acceptable selectivity index (SI = 27). Compounds I(R = 2-pyrimidyl, 2-acetylamino-4-thiozolyl, 2-imidazolyl) exhibited potent activity against T. brucei rhodesiense (IC50 = 12-60 nM). Ten of the 15 compounds with pyrimidine, pyrrole, thiazole and imidazole terminal units were highly active against P. falciparum (IC50 = 9-87 nM). Both pyrimidine and pyridine terminal groups are advantageous for anti-T. cruzi activity and several different heterocyclic terminal units are effective vs. P. falciparum, both findings merit further investigation.
European Journal of Medicinal Chemistry published new progress about 4604-72-2. 4604-72-2 belongs to pyrazines, auxiliary class Pyrazine,Amine,Amide, name is Pyrazine-2-carbothioamide, and the molecular formula is C5H5N3S, Computed Properties of 4604-72-2.
Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem