1267638-65-2

Upstream product

• 655250-09-2 N₈-(4-amino-1-methylpentyl)-2-tert-butyl-6-methoxy-8-quinolinamine 
• 2480-93-5 (R)-Nδ-benzyloxycarbonyl-Nα-(tert-butoxycarbonyl)-ornithine 
• 1267638-49-2 benzyl ((4R)-4-amino-5-[(4-((2-tert-butyl-6-methoxyquinolin-8-yl)amino)pentyl)amino]-5-oxopentyl)carbamate 
• 530-62-1 1,1'-carbonyldiimidazole 
• 1267638-34-5 benzyl [(4R)-4-[(tert-butoxycarbonyl)amino]-5-((4-[(2-tert-butyl-6-methoxyquinolin-8-yl)-amino]pentyl)amino)-5-oxopentyl]-carbamate 

Relevant academic research and scientific papers

Synthesis, antiprotozoal, antimicrobial, β-hematin inhibition, cytotoxicity and methemoglobin (MetHb) formation activities of bis(8-aminoquinolines)

In continuing our search of potent antimalarials based on 8-aminoquinoline structural framework, three series of novel bis(8-aminoquinolines) using convenient one to four steps synthetic procedures were synthesized. The bisquinolines were evaluated for in vitro antimalarial (Plasmodium falciparum), antileishmanial (Leishmania donovani), antimicrobial (a panel of pathogenic bacteria and fungi), cytotoxicity, β-hematin inhibitory and methemoglobin (MetHb) formation activities. Several compounds exhibited superior antimalarial activities compared to parent drug primaquine. Selected compounds (44, 61 and 79) when tested for in vivo blood-schizontocidal antimalarial activity (Plasmodium berghei) displayed potent blood-schizontocial activities. The bisquinolines showed negligible MetHb formation (0.2-1.2%) underlining their potential in the treatment of glucose-6-phosphate dehydrogenase deficient patients. The bisquinoline analogues (36, 73 and 79) also exhibited promising in vitro antileishmanial activity, and antimicrobial activities (43, 44 and 76) against a panel of pathogenic bacteria and fungi. The results of this study provide evidence that bis(8-aminoquinolines), like their bis(4-aminoquinolines) and artemisinin dimers counterparts, are a promising class of antimalarial agents.