219624-82-5

Upstream product

• 473421-00-0 (R)-2-Amino-3-cyclohexylmethylsulfanyl-propionic acid 
• 2550-36-9 Cyclohexylmethyl bromide 
• 24424-99-5 di-tert-butyl dicarbonate 
• 2393-23-9 4-methoxy-benzylamine 
• 219626-94-5 (2R)-2-(t-butoxycarbonylamino)-3-cyclohexylmethylthiopropanoic acid 

Downstream Products

• 219626-08-1 (2R)-N-(4-methoxybenzyl)-3-cyclohexylmethylsulfonyl-2-t-butoxycarbonyl-aminopropanamide 
• 219625-66-8 (2R)-N-(4-methoxybenzyl)-3-cyclohexylmethylthio-2-((4R)-3-t-butoxycarbonyl-thiazolidin-4-ylcarbonylamino)propanamide 
• 473421-31-7 2-amino-3-cyclohexylmethylsulfanyl-N-(4-methoxy-benzyl)-propionamide 

Relevant academic research and scientific papers

Amino acid derivatives

A compound of the formula (1): [wherein R1 is (substituted) alkyl, alkoxy, phenyl, hetero ring etc.; A is bond, CO, SO2; R2 is H, (substituted) alkyl etc.; D is alkylene etc.; E is COO, OCO, O, S, SO, SO2 etc.;

Structure-activity study of L-amino acid-based N-type calcium channel blockers

Synthesis and structure-activity relationship (SAR) study of L-amino acid-based N-type calcium channel blockers are described. The compounds synthesized were evaluated for inhibitory activity against both N-type and L-type calcium channels focusing on sel

Structure-activity study of L-cysteine-based N-type calcium channel blockers: optimization of N- and C-terminal substituents.

Synthesis and structure-activity relationship (SAR) studies of L-cysteine-based N-type calcium channel blockers are described. In the course of exploring SAR of the N- and C-terminal substituents, the L-cysteine derivative was found to be a potent N-type calcium channel blocker with an IC(50) value of 0.14 microM on IMR-32 assay. Compound showed 12-fold selectivity for N-type over L-type calcium channels on AtT-20 assay.

Structure-activity study and analgesic efficacy of amino acid derivatives as N-type calcium channel blockers

The synthesis and structure-activity relationship (SAR) study of a novel series of N-type calcium channel blockers are described. L-Cysteine derivative 2a was found to be a potent and selective N-type calcium channel blocker with IC50 0.63 μM on IMR-32 assay. Compound 2a showed analgesic efficacy in the rat formalin-induced pain model by intrathecal and oral administration.