1310682-46-2

Upstream product

• 95-76-1 m,p-dichloroaniline 
• 58482-93-2 tert-butylaminoacetic acid 
• 36668-76-5 tert-butyl cyanamide 
• 1310682-73-5 C₈H₁₄N₂OS 
• 65783-10-0 N-(3,4-dichlorophenyl)guanidine 
• 1310682-69-9 1-tert-butyl-2-thioxoimidazolidin-4-one 
• 1310682-75-7 2-amino-1-tert-butyl-1,5-dihydroimidazol-4-one 
• 18995-48-7 N-(3,4-dichlorophenyl)cyanamide 

Downstream Products

• 1310682-49-5 N-(tert-butoxycarbonyl)-N'-(3,4-dichlorophenyl)-N''-(1-tert-butyl-4-oxo-4,5-dihydro-1H-imidazol-2-yl)guanidine 

Relevant academic research and scientific papers

2-GUANIDINO-4-OXO-IMIDAZOLINE DERIVATIVES AS ANTIMALARIAL AGENTS, SYNTHESIS AND METHODS OF USE THEREOF

The present invention relates to new 2-guanidino-4-oxo-imidazoline derivatives (deoxo-IZ), methods of making these compounds, compositions containing the same, and methods of using the same to prevent, treat, or inhibit malaria in a subject.

Synthesis and antimalarial activity of 2-guanidino-4-oxoimidazoline derivatives

A series of 2-guanidino-4-oxoimidazoline (deoxo-IZ) derivatives was prepared and showed potent antimalarial activities in rodent and Rhesus models. Compound 8e, the most potent analogues of this series, is the first non-8-aminoqinoline antimalarial that demonstrated radical curative activity in non-human primate by oral route and showed causal prophylactic activity comparable to that of the commonly used clinical drugs in Rhesus monkeys infected with sporozoites of Plasmodium cynomolgi. The metabolic stability and metabolites profile indicated that the new deoxo-IZ derivatives (8) may act as prodrugs of the corresponding IZ (1 and 2) derivatives.