706803-45-4

Upstream product

• 98760-08-8 (1-oxiranyl-2-phenylethyl)carbamic acid tert-butyl ester 
• 99-27-4 dimethyl 5-aminoisophthalate 
• 911790-36-8 5-(1,1-dioxo-[1,2]thiazinan-2-yl)isophthalic acid monomethyl ester 
• 911790-35-7 C₁₄H₁₇NO₆S 
• 149451-80-9 (2S,3S)-3-(t-butoxycarbonylamino)-4-phenylbutane-1,2-diol 
• 103127-52-2 ((S)-1-benzylallyl)carbamic acid tert-butyl ester 
• 109138-28-5 1-(3-methoxyphenyl)-1-methylethylamine 
• 706795-10-0 C₂₀H₂₈N₂O₂ 
• 1349180-49-9 5-(1,1-dioxo-[1,2]thiazinan-2-yl)-N,N-dipropylisophthalamic acid 
• 1349188-02-8 5-(1,1-dioxo-[1,2]thiazinan-2-yl)-N,N-dipropylisophthalamic acid methyl ester 

Relevant academic research and scientific papers

Plasmepsin inhibitory activity and structure-guided optimization of a potent hydroxyethylamine-based antimalarial hit

Antimalarial hit 1SR (TCMDC-134674) identified in a GlaxoSmithKline cell based screening campaign was evaluated for inhibitory activity against the digestive vacuole plasmepsins (Plm I, II, and IV). It was found to be a potent Plm IV inhibitor with no selectivity over Cathepsin D. A cocrystal structure of 1SR bound to Plm II was solved, providing structural insight for the design of more potent and selective analogues. Structure-guided optimization led to the identification of structurally simplified analogues 17 and 18 as low nanomolar inhibitors of both, plasmepsin Plm IV activity and P. falciparum growth in erythrocytes.