1403479-91-3

Upstream product

• 1403479-89-9 (R)-methyl 3-((tert-butyldimethylsilyl)oxy)-4-(4-fluoro-N-methylphenylsulfonamido)butanoate 
• 1403482-02-9 (R)-methyl 4-amino-3-((tert-butyldimethylsilyl)oxy)butanoate 
• 1403479-90-2 (R)-methyl 3-((tertbutyldimethylsilyl)oxy)-4-(4-fluorophenylsulfonamido)butanoate 
• 18162-48-6 tert-butyldimethylsilyl chloride 

Downstream Products

• 1403480-26-1 N-((R)-3-((tert-butyldimethylsilyl)oxy)-4-(4-fluoro-N-methylphenylsulfonamido)butyl)-N-((S)-1-((4-methoxybenzyl)oxy)propan-2-yl)-5-nitro-2-((S)-pent-4-en-2-yloxy)benzamide 
• 1403480-66-9 N-((R)-4-(4-fluoro-N-methylphenylsulfonamido)-3-hydroxybutyl)-N-((S)-1-((4-methoxybenzyl)oxy)propan-2-yl)-5-nitro-2-((S)-pent-4-en-2-yloxy)benzamide 
• 1403480-86-3 N-((R)-3-(allyloxy)-4-(4-fluoro-N-methylphenylsulfonamido)butyl)-N-((S)-1-((4-methoxybenzyl)oxy)propan-2-yl)-5-nitro-2-((S)-pent-4-en-2-yloxy)benzamide 
• 1403479-02-6 N-(((2S,8R)-14-(3-(3,5-dimethylisoxazol-4-yl)ureido)-11-((2S)-1-((4-methoxybenzyl)oxy)propan-2-yl)-2-methyl-12-oxo-2,3,4,5,6,8,9,10,11,12-decahydrobenzo[b][1,9,5]dioxaazacyclotetradecin-8-yl)methyl)-4-fluoro-N-methylbenzenesulfonamide 
• 1403480-00-1 N-((R)-2-((tert-butyldimethylsilyl)oxy)-4-(((S)-1-((4-methoxybenzyl)oxy)propan-2-yl)amino)butyl)-4-fluoro-N-methylphenylsulfonamide 
• 1403479-96-8 (R)-3-((tert-butyldimethylsilyl)oxy)-4-(4-fluoro-N-methylphenylsulfonamido)-N-((S)-1-((4-methoxybenzyl)oxy)propan-2-yl)butanamide 

Relevant academic research and scientific papers

Diversity-oriented synthesis-facilitated medicinal chemistry: Toward the development of novel antimalarial agents

Here, we describe medicinal chemistry that was accelerated by a diversity-oriented synthesis (DOS) pathway, and in vivo studies of our previously reported macrocyclic antimalarial agent that derived from the synthetic pathway. Structure-activity relationships that focused on both appendage and skeletal features yielded a nanomolar inhibitor of P. falciparum asexual blood-stage growth with improved solubility and microsomal stability and reduced hERG binding. The build/couple/pair (B/C/P) synthetic strategy, used in the preparation of the original screening library, facilitated medicinal chemistry optimization of the antimalarial lead.

MACROLACTAM COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA

The present invention relates to a macrolactam compound, and methods for treating a subject with malaria using the macrolactam compound, represented by the following structural formula (l), wherein the values and preferred values of the variables are defined herein.