6938-02-9

Upstream product

• 5333-02-8 5,6-dimethoxy-8-nitroquinoline 
• 7595-31-5 4-amino-5-nitroveratrol 
• 99069-17-7 4-Acetylamino-1,2-dimethoxy-5-nitrobenzene 
• 5347-15-9 5-bromo-6-methoxy-8-nitroquinoline 
• 3395-03-7 4,5-dimethoxy-1,2-dinitrobenzene 
• 85-81-4 6-methoxy-8-nitroquinoline 

Downstream Products

• 17605-92-4 8-amino-quinoline-5,6-diol 
• 132247-40-6 N-(5,6-Dimethoxy-quinolin-8-yl)-benzamide 
• 132247-41-7 4-Chloro-N-(5,6-dimethoxy-quinolin-8-yl)-benzamide 
• 132247-42-8 4-Bromo-N-(5,6-dimethoxy-quinolin-8-yl)-benzamide 
• 132247-43-9 Cyclohexanecarboxylic acid (5,6-dimethoxy-quinolin-8-yl)-amide 
• 132247-47-3 N-(5,6-Dioxo-5,6-dihydro-quinolin-8-yl)-benzamide 
• 132247-50-8 Cyclohexanecarboxylic acid (5,6-dioxo-5,6-dihydro-quinolin-8-yl)-amide 
• 132247-48-4 4-Chloro-N-(5,6-dioxo-5,6-dihydro-quinolin-8-yl)-benzamide 
• 132247-49-5 4-Bromo-N-(5,6-dioxo-5,6-dihydro-quinolin-8-yl)-benzamide 
• 87321-06-0 5-hydroxy-6-desmethylprimaquine 
• 5423-91-6 N-(5,6-dimethoxy-[8]quinolyl)-hexanediyldiamine 
• 7505-76-2 N-(5,6-Dioxo-5,6-dihydro-quinolin-8-yl)-acetamide 
• 132247-35-9 8-Ethylamino-quinoline-5,6-dione 
• 49797-49-1 8-Amino-5,6-quinolinedione 

Relevant academic research and scientific papers

Antimalarial activity of primaquine operates via a two-step biochemical relay

Primaquine (PQ) is an essential antimalarial drug but despite being developed over 70 years ago, its mode of action is unclear. Here, we demonstrate that hydroxylated-PQ metabolites (OH-PQm) are responsible for efficacy against liver and sexual transmission stages of Plasmodium falciparum. The antimalarial activity of PQ against liver stages depends on host CYP2D6 status, whilst OH-PQm display direct, CYP2D6-independent, activity. PQ requires hepatic metabolism to exert activity against gametocyte stages. OH-PQm exert modest antimalarial efficacy against parasite gametocytes; however, potency is enhanced ca.1000 fold in the presence of cytochrome P450 NADPH:oxidoreductase (CPR) from the liver and bone marrow. Enhancement of OH-PQm efficacy is due to the direct reduction of quinoneimine metabolites by CPR with the concomitant and excessive generation of H2O2, leading to parasite killing. This detailed understanding of the mechanism paves the way to rationally re-designed 8-aminoquinolines with improved pharmacological profiles.

HEAT SHOCK PROTEIN 90 INHIBITORS, METHODS OF PREPARING SAME, AND METHODS FOR THEIR USE

Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors are disclosed. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases and conditions, such as inflammation and neurodegenerative disorders. Methods of treating and preventing cancer and other Hsp90 related diseases and conditions are disclosed that include administering to the subject a therapeutically effective amount of an Hsp90 inhibitor. Methods of preparing the novel Hsp90 inhibitors are also provided.

8-Aminoquinolines as anticoccidials - I

The proposed ring metabolites of the 8-aminoquinoline antimalarial, pentaquine, 1, have been synthesised and their biological activity as anticoccidial agents investigated in vivo. Several analogues in which this metabolic pathway had been blocked were also synthesised and their anticoccidial activity measured.

Antimalarials. 13. 5-Alkoxy Analogues of 4-Methylprimaquine

A series of nuclear and side-chain analogues of 4-methylprimaquine incorporating an alkoxy group in 5-position of the quinoline nucleus has been prepared.The compounds were tested for suppresive antimalarial activity against Plasmodium berghei in mice and for radical curative antimalarial activity against Plasmodium cynomolgi in the rhesus monkey.Although the toxicity problems characteristic of the 8-aminoquinolines were not overcome, several of the compounds, suprisingly, were highly effective as both blood and tissue schizonticidal agents.