951890-84-9

Upstream product

• 89794-02-5 4-bromo-2-chlorotoluene 
• 587-04-2 m-Chlorobenzaldehyde 

Downstream Products

• 1392422-01-3 C₂₈H₂₇Cl₂N₃O₂ 
• 1050527-04-2 (+/-)-N-{[3-chloro-4-(pyrrolidin-1-ylmethyl)phenyl](3-chlorophenyl)methyl}-7-trifluoromethyl-4-aminoquinoline 
• 1050527-48-4 (3-chlorophenyl)(4-methyl-3-chlorophenyl)methanone 
• 1050527-61-1 (3-chlorophenyl)(3-chloro-4-(pyrrolidin-1-ylmethyl)phenyl)methanone 
• 1050527-63-3 (3-chlorophenyl)(3-chloro-4-(morpholin-4-ylmethyl)phenyl)methanone 
• 1392422-06-8 (3-chlorophenyl)(3-chloro-4-(1-tert-butoxycarbonylpiperazin-4-ylmethyl)phenyl)methanone 
• 1050527-69-9 [3-chloro-4-(pyrrolidin-1-ylmethyl)phenyl](3-chlorophenyl)methanone oxime 
• 1050527-81-5 (3-chlorophenyl)(3-chloro-4-(pyrrolidin-1-ylmethyl)phenyl)methanamine 
• 1050527-83-7 (3-chlorophenyl)(3-chloro-4-(morpholin-4-ylmethyl)phenyl)methanone 
• 1392422-10-4 (3-chlorophenyl)(3-chloro-4-(1-tert-butoxycarbonylpiperazin-4-ylmethyl)phenyl)methanamine 
• 1392421-92-9 C₃₆H₂₉Cl₄N₅ 
• 1050526-93-6 (+/-)-7-chloro-N-{[3-chloro-4-(pyrrolidin-1-ylmethyl)phenyl](3-chlorophenyl)methyl}-4-aminoquinoline 
• 1050526-96-9 (+/-)-7-chloro-N-{[3-chloro-4-(morpholin-4-ylmethyl)phenyl](3-chlorophenyl)methyl}-4-aminoquinoline 
• 1050527-15-5 (+/-)-N-{[3-chloro-4-(pyrrolidin-1-ylmethyl)phenyl](3-chlorophenyl)methyl}-6-methoxy-4-aminoquinoline 

Relevant academic research and scientific papers

Optimization of 4-aminoquinoline/clotrimazole-based hybrid antimalarials: Further structure-activity relationships, in vivo studies, and preliminary toxicity profiling

Despite recent progress in the fight against malaria, the emergence and spread of drug-resistant parasites remains a serious obstacle to the treatment of infections. We recently reported the development of a novel antimalarial drug that combines the 4-aminoquinoline pharmacophore of chloroquine with that of clotrimazole-based antimalarials. Here we describe the optimization of this class of hybrid drug through in-depth structure-activity relationship studies. Antiplasmodial properties and mode of action were characterized in vitro and in vivo, and interactions with the parasites 'chloroquine resistance transporter' were investigated in a Xenopus laevis oocyte expression system. These tests indicated that piperazine derivatives 4b and 4d may be suitable for coadministration with chloroquine against chloroquine-resistant parasites. The potential for metabolism of the drugs by cytochrome P450 was determined in silico, and the lead compounds were tested for toxicity and mutagenicity. A preliminary pharmacokinetic analysis undertaken in mice indicated that compound 4b has an optimal half-life.

NOVEL 4-AMINO-QUINOLINE DERIVATIVES USEFUL AS ANTI-MALARIA DRUGS

The present invention relates to clotrimazole/quinoline hybrids useful as active ingredients of anti-malaria drugs. The compounds show a remarkable in vitro biological activity especially against the chloroquine-resistant Plasmodium falciparum strains and

NOVEL 4-AMINO-QUINOLINE DERIVATIVES USEFUL AS ANTI-MALARIA DRUGS

The present invention relates to clotrimazole/quinoline hybrids useful as active ingredients of anti-malaria drugs. The compounds show a remarkable in vitro biological activity especially against the chloroquine-resistant Plasmodium falciparum strains and