911790-36-8

Upstream product

• 1633-84-7 4-chloro-1-butanesulfonyl chloride 
• 99-27-4 dimethyl 5-aminoisophthalate 
• 911790-35-7 C₁₄H₁₇NO₆S 

Downstream Products

• 1349188-02-8 5-(1,1-dioxo-[1,2]thiazinan-2-yl)-N,N-dipropylisophthalamic acid methyl ester 
• 1349180-49-9 5-(1,1-dioxo-[1,2]thiazinan-2-yl)-N,N-dipropylisophthalamic acid 
• 706803-45-4 N-{(1S,2R)-1-benzyl-2-hydroxy-3-[1-(3-methoxyphenyl)-1-methylethylamino]propyl}-5-(1,1-dioxo-[1,2]thiazinan-2-yl)-N',N'-dipropylisophthalamide 
• 1539276-54-4 N-{(1S,2S)-1-benzyl-2-hydroxy-3-[1-(3-methoxyphenyl)-1-methylethylamino]propyl}-5-(1,1-dioxo-[1,2]thiazinan-2-yl)-N',N'-dipropylisophthalamide 
• 1539276-55-5 N-[(1S,2R)-1-benzyl-2-hydroxy-3-(1-methyl-1-phenylethylamino)propyl]-5-(1,1-dioxo-[1,2]thiazinan-2-yl)-N',N'-dipropylisophthalamide 
• 1539276-56-6 N-[(1S,2S)-1-benzyl-2-hydroxy-3-(1-methyl-1-phenylethylamino)propyl]-5-(1,1-dioxo-[1,2]thiazinan-2-yl)-N',N'-dipropylisophthalamide 
• 1539276-45-3 N-[(1S,2R)-1-benzyl-2-hydroxy-3-(3-methoxybenzylamino)propyl]-5-(1,1-dioxo-[1,2]thiazinan-2-yl)-N',N'-dipropylisophthalamide 

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.

Substituted 1,2-ethylenediamines, Methods for Preparing Them and Uses Thereof

The present invention relates to substituted 1,2-ethylenediamines of general formula (I) wherein the groups R1 to R15, A, B, L, i as well as X1-X4 are defined as in the specification and claims and the use thereof for the treatment of Alzheimer's disease (AD) and similar diseases.