70922-92-8

Upstream product

• 574-98-1 2-(2-bromoethyl)isoindoline-1,3-dione 
• 622-33-3 N-benzyloxyamine 
• 100-51-6 benzyl alcohol 

Downstream Products

• 70922-93-9 N-(benzyloxy)-ethylene-diamine 
• 70923-05-6 1-benzyloxy-3-(2,6-dichlorophenyl)-1-(2-phthalimidoethyl)-2-thiourea 
• 70993-56-5 1-benzyloxy-3-(3,4-dimethoxyphenyl)-1-(2-phthalimidoethyl)2-thiourea 
• 82401-37-4 1-(benzyloxy)-3-(2-chloro-5-methoxyphenyl)-1-(2-phthalimidoethyl)-2-thiourea 
• 82401-32-9 1-(benzyloxy)-3-(2,6-difluorophenyl)-1-(2-phthalimidoethyl)-2-thiourea 
• 70923-31-8 1-benzyloxy-3-(3,4-dimethylphenyl)-1-(2-phthalimidoethyl)-2-thiourea 
• 265655-42-3 N-benzyloxy-N-(2'-phtalimidoethyl)-3-phtalimido-propanamide 

Relevant academic research and scientific papers

Synthesis and antiprotozoal activity of n -alkoxy analogues of the trypanocidal lead compound 4,4′-bis(imidazolinylamino)diphenylamine with improved human blood-brain barrier permeability

To improve the blood-brain barrier permeability of the trypanocidal lead compound 4,4′-bis(imidazolinylamino)diphenylamine (1), five N-alkoxy analogues were synthesized from bis(4-isothiocyanatophenyl)amine and N-alkoxy-N-(2-aminoethyl)-2-nitrobenzenesulfonamides following successive chemical reactions in just one reactor (one-pot procedure). This involved: (a) formation of a thiourea intermediate, (b) removal of the amine protecting groups, and (c) intramolecular cyclization. The blood-brain barrier permeability of the compounds determined in vitro by transport assays through the hCMEC/D3 human cell line, a well-known and characterized human cellular blood-brain barrier model, showed that the N-hydroxy analogue 16 had enhanced blood-brain barrier permeability compared with the unsubstituted lead compound. Moreover, this compound displayed low micromolar IC50 against Trypanosoma brucei rhodesiense and Plasmodium falciparum and moderate activity by intraperitoneal administration in the STIB900 murine model of acute sleeping sickness.

1-Benzyloxy-4,5-dihydro-1H-imidazol-2-yl-amines, a novel class of NR1/2B subtype selective NMDA receptor antagonists

Screening of the Roche compound depository led to the identification of (1-benzyloxy-4,5-dihydro-1H-imidazol-2-yl)-butyl amine 4, a structurally novel NR1/2B subtype selective NMDA receptor antagonist. The structure-activity relationships developed in this series resulted in the discovery of a novel class of potent and selective NMDA receptor blockers displaying activity in vivo.

2-Imino-imidazolidine derivatives

2-Imino-imidazolidine derivatives of the formula STR1 wherein R1, R2, R3 and R4 are as hereinafter set forth, and pharmaceutically acceptable acid addition salts thereof, are described. The 2-imino-imidazolidine derivatives are useful in the treatment of hypertension.