1255397-71-7

Upstream product

• 103-71-9 phenyl isocyanate 
• 1353557-67-1 C₃₇H₅₀N₄O₆ 
• 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 
• 1333331-62-6 C₃₇H₅₃N₃O₉ 
• 1333331-60-4 C₃₄H₄₉N₃O₉ 
• 1333331-58-0 C₄₀H₆₃N₃O₉Si 
• 1353557-62-6 C₃₆H₄₆N₄O₆ 
• 1353557-61-5 (S)-2-((2S,8R,9R)-8-((((allyloxy)carbonyl)(methyl)amino)methyl)-2,9-dimethyl-12-oxo-14-(3-phenylureudo)-3,4,5,6,9,10-hexahydrobenzo[b][1,9,5]dioxaazacyclotetradecin-11(2H,8H,12H)-yl)propyl benzoate 
• 1353557-59-1 (S)-2-((2S,8R,9R)-14-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)-8-((((allyloxy)carbonyl)(methyl)amino)methyl)-2,9-dimethyl-12-oxo-3,4,5,6,9,10-hexahydrobenzo[b][1,9,5]dioxaazacyclotetradecin-11(2H,8H,12H)-yl)propyl benzoate 
• 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 
• 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 
• 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 
• 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 
• 1255214-08-4 allyl (((2S,8R,9R)-14-((((9H-fIuoren-9-yl)methoxy)carbonyl)amino)-11-((S)-1-hydroxypropan-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)(methyl)carbamate 

Downstream Products

• 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 
• 1353557-48-8 (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 
• 1403479-53-7 3-[(2S,8R,9R)-11-[(2S)-1-methoxypropan-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-benzodioxazacyclotetradecin-14-yl]-1-phenylurea 
• 1403479-55-9 3-[(2S,8R,9R)-11-[(2S)-1-[(tert-butyldimethylsilyl)oxy]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-benzodioxazacyclotetradecin-14-yl]-1-phenylurea 
• 1403479-58-2 (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-benzodioxazacyclotetradecin-11-yl]propyl 4-methylbenzene-1-sulfonate 
• 1403479-51-5 3-[(2S,8R,9R)-2,9-dimethyl-8-{[N-methyl(4-fluorobenzene)sulfonamido]methyl}-12-oxo-11-[(2S)-1-(pyridin-3-yloxy)propan-2-yl]-2,3,4,5,6,8,9,10,11,12-decahydro-1,7,11-benzodioxazacyclotetradecin-14-yl]-1-phenylurea 

Relevant academic research and scientific papers

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.

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.