91558-02-0

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 459-73-4 GlyOEt*HCl 
• 100-46-9 benzylamine 
• 623-33-6 glycine ethyl ester hydrochloride 
• 3173-56-6 benzyl isothiocyanate 
• 2949-22-6 Glycine ethyl ester isocyanate 

Downstream Products

• 67909-04-0 1-benzyl-1,3-dihydro-2H-imidazol-2-one 

Relevant academic research and scientific papers

Small Molecule Inhibitors of Cyclophilin D to Protect Mitochondrial Function as a Potential Treatment for Acute Pancreatitis

Opening of the mitochondrial permeability transition pore (MPTP) causes mitochondrial dysfunction and necrosis in acute pancreatitis (AP), a condition without specific drug treatment. Cyclophilin D (CypD) is a mitochondrial matrix peptidyl-prolyl isomerase that regulates the MPTP and is a drug target for AP. We have synthesized urea-based small molecule inhibitors of cyclophilins and tested them against CypD using binding and isomerase activity assays. Thermodynamic profiles of the CypD/inhibitor interactions were determined by isothermal titration calorimetry. Seven new high-resolution crystal structures of CypD-inhibitor complexes were obtained to guide compound optimization. Compounds 4, 13, 14, and 19 were tested in freshly isolated murine pancreatic acinar cells (PACs) to determine inhibition of toxin-induced loss of mitochondrial membrane potential (δΨm) and necrotic cell death pathway activation. Compound 19 was found to have a Kd of 410 nM and a favorable thermodynamic profile, and it showed significant protection of δΨm and reduced necrosis of murine as well as human PACs. Compound 19 holds significant promise for future lead optimization.

NEW INHIBITORS OF CYCLOPHILINS AND USES THEREOF

The present invention relates to a compound of formula (I): Formula (I), wherein: - n is 0, 1 or 2; - A is in particular CH or N; - X is in particular CO, SO2, CS, and R1 is in particular H, - R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, - R6 is in particular H or an alkyl group, and - R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.

HMG-CoA reductase inhibitors

Compounds are provided of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and trea

Isocyanates, Part 4.10 Convenient Phosgene-Free Method for the Synthesis and Derivatization of Enantiopure α-Isocyanato Carboxylic Acid Esters

A novel phosgene-free procedure for the synthesis of α-isocyanato carboxylic acid esters starting from α-amino acid esters has been achieved. The isocyanates are obtained enantiomerically pure (> 99% ee) by a DMAP-catalyzed isocyanation with di-tert-butyl