Devine, William; Thomas, Sarah M.; Erath, Jessey; Bachovchin, Kelly A.; Lee, Patricia J.; Leed, Susan E.; Rodriguez, Ana; Sciotti, Richard J.; Mensa-Wilmot, Kojo; Pollastri, Michael P. published the artcile< Antiparasitic Lead Discovery: Toward Optimization of a Chemotype with Activity Against Multiple Protozoan Parasites>, Recommanded Product: Pyridazin-4-amine, the main research area is trypanosomicide leishmanicide antimalarial development NEU1045 analog preparation pharmacokinetics; Antiparasitic agents; Chagas disease; Leishmania major; Plasmodium falciparum; Trypanosoma brucei; Trypanosoma cruzi; human African trypanosomiasis; leishmaniasis.
Human African trypanosomiasis (HAT), Chagas disease, and leishmaniasis present a significant burden across the developing world. Existing therapeutics for these protozoal neglected tropical diseases suffer from severe side effects and toxicity. Previously, NEU-1045 was identified as a promising lead with cross-pathogen activity, though it possessed poor physicochem. properties. The authors have designed a library of analogs with improved calculated physicochem. properties built on the quinoline scaffold of 3 incorporating small, polar aminoheterocycles in place of the 4-(3-fluorobenzyloxy)aniline substituent. The authors report the biol. activity of these inhibitors against Trypanosoma brucei (HAT), T. cruzi (Chagas disease), and Leishmania major (cutaneous leishmaniasis), and describe the identification of N-(5-chloropyrimidin-2-yl)-6-(4-(morpholinosulfonyl)phenyl)quinolin-4-amine (13t) as a promising inhibitor of L. major proliferation and 6-(4-(morpholinosulfonyl)phenyl)-N-(pyrimidin-4-yl)quinolin-4-amine (13j), a potent inhibitor of T. brucei proliferation with improved drug-like properties.
ACS Medicinal Chemistry Letters published new progress about Antimalarials. 20744-39-2 belongs to class pyridazine, and the molecular formula is C4H5N3, Recommanded Product: Pyridazin-4-amine.
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem