Related Products of 57825-30-6. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 1-(Bromomethyl)-4-ethylbenzene, is researched, Molecular C9H11Br, CAS is 57825-30-6, about Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors. Author is Buchynskyy, Andriy; Gillespie, J. Robert; Hulverson, Matthew A.; McQueen, Joshua; Creason, Sharon A.; Ranade, Ranae M.; Duster, Nicole A.; Gelb, Michael H.; Buckner, Frederick S..
A phenotypic screen of a compound library for antiparasitic activity on Trypanosoma brucei, the causative agent of Human African Trypanosomiasis (HAT), led to the identification of N-(2-aminoethyl)-N-Ph benzamides as a starting point for hit-to-lead medicinal chem. Eighty two analogs were prepared, which led to the identification of a set of highly potent N-(2-aminoethyl)-N-benzyloxyphenyl benzamides with the most potent compound 73 having an in vitro EC50 = 0.001 μM. The compounds displayed drug-like properties when tested in a number of in vitro assays. Compound 73 was orally bioavailable and displayed good plasma and brain exposure in mice, cured 2 out of 3 mice infected with Trypanosoma brucei in acute model when dosed orally at 50 mg/kg once per day for 4 days. Given its potent antiparasitic properties and its ease of synthesis, compound 73 represents a potential lead for the development of drug to treat Human African Trypanosomiasis.
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Reference:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider