1333331-60-4

Upstream product

• 1333331-58-0 C₄₀H₆₃N₃O₉Si 
• 1255212-85-1 tert-butyl((2R,3R)-2-((tert-butyldimethylsilyl)oxy)-4-(((S)-1-((4-methoxybenzyl)oxy)propan-2-yl)amino)-3-methylbutyl)(methyl)carbamate 
• 1255213-22-9 C₁₂H₁₃NO₅ 

Downstream Products

• 1333331-64-8 tert-butyl (((2S,8R,9R)-11-((S)-1-((4-methoxybenzyl)oxy)propan-2-yl)-2,9-dimethyl-14-nitro-12-oxo-2,3,6,8,9,10,11,12-octahydrobenzo[b][1,9,5]dioxaazacyclotetradecin-8-yl)methyl)(methyl)carbamate 
• 1333331-66-0 tert-butyl (((2S,8R,9R)-14-amino-11-((S)-1-((4-methoxybenzyloxy)prop-2-yl)-2,9-dimethyl-12-oxo-2,3,4,5,6,8,9,10,11,12-ecahydrobenzo[b][1,9,5]dioxaazacyclotetradec-8-yl)methyl)-methyl)carbamate 
• 1353557-47-7 2-fluoro-N-(((2S,8R,9R)-11-((S)-1-((4-methoxybenzyl)oxy)propan-2-yl)-2,9-dimethyl-12-oxo-14-(3-phenylureudo)-2,3,4,5,6,8,9,10,11,12-decahydrobenzo[b][1,9,5]dioxaazacyclotetradecin-8-yl)methyl)-N-methylbenzenesulfonamide 
• 1255397-71-7 3-[(2S,8R,9R)-11-((S)-1-hydroxypropan-2-yl)-2,9-dimethyl-8-[(N-methyl(4-fluorobenzene)sulfonamido)methyl]-12-oxo-2,3,4,5,6,8,9,10,11,12-decahydro-1,7,11-benzodioxaazacyclotetradecin-14-yl]-1-phenylurea 
• 1353557-48-8 (2S)-2-[(2S,8R,9R)-2,9-dimethyl-8-[(N-methyl(4-fluorobenzene)sulfonamido)methyl]-12-oxo-14-[(phenylcarbamoyl)amino]-2,3,4,5,6,8,9,10,11,12-decahydro-1,7,11-benzodioxaazacyclotetradecin-11-yl]propyl 2,2-dimethylpropanoate 
• 1353557-50-2 3-[(2S,8R,9R)-11-[(S)-1-(methoxymethyl)propan-2-yl]-2,9-dimethyl-8-[(N-methyl(4-fluorobenzene)sulfonamido)methyl]-12-oxo-2,3,4,5,6,8,9,10,11,12-decahydro-1,7,11-benzodioxaazacyclotetradecin-14-yl]-1-phenylurea 
• 1353557-51-3 N-(((2S,8R,9R)-11-((S)-1-azidopropan-2-yl)-2,9-dimethyl-12-oxo-14-(3-phenylureudo)-2,3,4,5,6,8,9,10,11,12-decahydrobenzo[b][1,9,5]dioxaazacyclotetradecin-8-yl)methyl)-4-fluoro-N-methylbenzenesulfonamide 
• 1353557-52-4 N-(((2S,8R,9R)-11-((S)-1-aminopropan-2-yl)-2,9-dimethyl-12-oxo-14-(3-phenylureudo)-2,3,4,5,6,8,9,10,11,12-decahydrobenzo[b][1,9,5]dioxaazacyclotetradecin-8-yl)methyl)-4-fluoro-N-methylbenzenesulfonamide 
• 1353557-53-5 3-[(2S,8R,9R)-2,9-dimethyl-8-[(N-methyl(4-fluorobenzene)sulfonamido)methyl]-11-[(S)-1-(methylamino)propan-2-yl]-12-oxo-2,3,4,5,6,8,9,10,11,12-decahydro-1,7,11-benzodioxaazacyclotetradecin-14-yl]-1-phenylurea 
• 1353557-64-8 tert-butyl (((2S,8R,9R)-11-((S)-1-((4-methoxybenzyl)oxy)propan-2-yl)-2,9-dimethyl-12-oxo-14-(3-phenylureido)-2,3,4,5,6,8,9,10,11,12-decahydrobenzo[b][1.9.5]dioxaazacyclotetradecin-8-yl)methyl)(methyl)carbamate 
• 1353557-67-1 C₃₇H₅₀N₄O₆ 
• 1353557-68-2 2-methoxyethyl (((2S,8R,9R)-11-((S)-1-((4-methoxybenzyl)oxy)propan-2-yl)-2,9-dimethyl-12-oxo-14-(3-phenylureido)-2,3,4,5,6,8,9,10,11,12-decahydrobenzo[b][1.9.5]dioxaazacyclotetradecin-8-yl)methyl)(methyl)carbamate 
• 1353557-69-3 N-(((2S,8R,9R)-14-(3-(3,5-dimethylisoxazol-4-yl)ureido)-11-((2S)-1-((4-methoxybenzyl)oxy)propan-2-yl)-2,9-dimethyl-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 
• 1333331-62-6 C₃₇H₅₃N₃O₉ 

Relevant academic research and scientific papers

Diversity-oriented synthesis yields a novel lead for the treatment of malaria

Here, we describe the discovery of a novel antimalarial agent using phenotypic screening of Plasmodium falciparum asexual blood-stage parasites. Screening a novel compound collection created using diversity-oriented synthesis (DOS) led to the initial hit. Structure-activity relationships guided the synthesis of compounds having improved potency and water solubility, yielding a subnanomolar inhibitor of parasite asexual blood-stage growth. Optimized compound 27 has an excellent off-target activity profile in erythrocyte lysis and HepG2 assays and is stable in human plasma. This compound is available via the molecular libraries probe production centers network (MLPCN) and is designated ML238.