1616684-82-2

Upstream product

• 368870-66-0 ethyl (R)-4-((tert-butoxycarbonyl)amino)-5-phenylpentanoate 
• 109-01-3 1-methyl-piperazine 
• 195867-20-0 (4S)-4-[(tert-butoxycarbonyl)amino]-5-phenylpentanoic acid 
• 124818-94-6 ethyl (2E,4S)-4-[(tert-butoxycarbonyl)amino]-5-phenylpent-2-enoate 
• 72155-45-4 Boc-L-phenylalaninal 
• 51987-73-6 (S)-2-tert-butoxycarbonylamino-3-phenyl-propionic acid methyl ester 
• 7524-50-7 methyl (2S)-2-amino-3-phenylpropanoate hydrochloride 
• 63-91-2 L-phenylalanine 

Downstream Products

• 1616684-83-3 (R)-4-amino-1-(4-methylpiperazin-1-yl)-5-phenylpentan-1-one 
• 1616684-84-4 (R)-4-(7-chloroquinolin-4-ylamino)-1-(4-methylpiperazin-1-yl)-5-phenylpentan-1-one 

Relevant academic research and scientific papers

Antiplasmodial activity of new 4-aminoquinoline derivatives against chloroquine resistant strain

Emergence and spread of multidrug resistant strains of Plasmodium falciparum has severely limited the antimalarial chemotherapeutic options. In order to overcome the obstacle, a set of new side-chain modified 4-aminoquinolines were synthesized and screened against chloroquine-sensitive (3D7) and chloroquine-resistant (K1) strains of P. falciparum. The key feature of the designed molecules is the use of methylpiperazine linked α, β3- and γ-amino acids to generate novel side chain modified 4-aminoquinoline analogues. Among the evaluated compounds, 20c and 30 were found more potent than CQ against K1 and displayed a four-fold and a three-fold higher activity respectively, with a good selectivity index (SI = 5846 and 11,350). All synthesized compounds had resistance index between 1.06 and >14.13 as against 47.2 for chloroquine. Biophysical studies suggested that this series of compounds act on heme polymerization target.