100618-81-3

Upstream product

• 1501-26-4 methyl 4-(chlorocarbonyl)butyrate 
• 1453473-39-6 methyl 5-(5-{2-[(methoxycarbonyl)amino]ethyl}thienyl)-5-oxopentanoate 
• 26011-68-7 methyl N-(2-phenylethyl)carbamate 

Downstream Products

• 1453473-47-6 9H-9-fluorenylmethyl N-{2-[4-(4-carboxybutyl)phenyl]ethyl} carbamate 
• 1453473-49-8 9H-9-fluorenylmethyl N-{2-[4-(5-amino-5-oxopentyl)phenyl]ethyl}carbamate 
• 1453473-52-3 9H-9-Fluorenylmethyl N-{2-[4-(4-aminobutyl)phenyl]ethyl} carbamate TFA salt 
• 1453474-37-7 C₂₈H₃₄N₄O₂ 
• 1453474-38-8 C₂₉H₃₆N₄O₂ 
• 1453474-40-2 C₃₁H₃₇N₅O₂ 
• 1453474-41-3 C₂₆H₃₄N₆O₂ 

Relevant academic research and scientific papers

Exploring the Polyamine Regulatory Site of the NMDA Receptor: A Parallel Synthesis Approach

The elongated structures of polyamine inverse agonists such as 1,12-diaminododecane (N12N) and 5-(4-aminobutyl)-2-thiopheneoctanamine (N4T8N) lend themselves to a combinatorial chemistry approach to explore a potential polyamine pharmacophore at the NMDA receptor. Herein we describe more than 100 new analogues of N4T8N obtained by breaking up the long octanamine arm into a dipeptide chain of equivalent length. Solid-phase parallel synthesis based on cross-linked polystyrene and a Wang anchor allowed the low-scale preparation of four small libraries based on the combination of two amino acid residues (out of Gly, Leu, Phe, Lys, phenylglycine, Tyr, Trp, His, and Arg). The obtained compounds were tested as modulators of [3H]MK-801 binding to rat brain membranes and of NMDA-induced currents in cultured rat hippocampal neurons. Compounds with two aromatic residues acted as binding inhibitors (inverse agonists). Compounds with two Lys residues acted as binding stimulators (agonists) and had stimulatory and inhibitory effects on NMDA-induced currents, depending on the holding potential. High sensitivity of binding inhibition to spermine was conferred by a Tyr residue, whereas a His residue favored high potency at acidic pH.

Sulphonamides containing a tetrazolyl radical

The present invention provides sulphonamides of the general formula: STR1 wherein R is a hydrogen or halogen arom, a cyano group or a C1 -C6 -alkyl or trifluoromethyl radical, n is 1, 2 or 3, m is 0 or 1 to 5, X is a valency bond, an oxygen atom, a carbonyl group or a --CHOH-- group, A is a valency bond or a carbonyl group and B is a valency bond or an --NH-- group; the physiologically acceptable salts thereof with inorganic and organic acids, as well as the optical isomers thereof. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.