88932-74-5

Upstream product

• 88932-71-2 4-{[N-(tert-butyloxycarbonyl)-L-phenylalanyl]amino}pyridine 
• 32150-91-7 phthaloyl-L-phenylalanyl chloride 
• 504-24-5 4-aminopyridine 
• 152611-65-9 (S)-α-phthalimido-N-(4-pyridyl)benzene propanamide 
• 13734-34-4 N-tert-butoxycarbonyl-L-phenylalanine 

Downstream Products

• 157560-35-5 {3-[(S)-2-Phenyl-1-(pyridin-4-ylcarbamoyl)-ethyl]-ureido}-acetic acid benzyl ester 
• 149047-42-7 (S)-N'-benzyl, N'-urea 
• 714970-07-7 (S)-2-[(S)-2-Phenyl-1-(pyridin-4-ylcarbamoyl)-ethylcarbamoyl]-pyrrolidine-1-carboxylic acid tert-butyl ester 
• 714970-64-6 ((S)-1-(4-Hydroxy-2,6-dimethyl-benzyl)-2-oxo-2-{(S)-2-[(S)-2-phenyl-1-(pyridin-4-ylcarbamoyl)-ethylcarbamoyl]-pyrrolidin-1-yl}-ethyl)-carbamic acid tert-butyl ester 
• 714970-33-9 ((S)-1-(4-Hydroxy-benzyl)-2-oxo-2-{(S)-2-[(S)-2-phenyl-1-(pyridin-4-ylcarbamoyl)-ethylcarbamoyl]-pyrrolidin-1-yl}-ethyl)-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

Chiral primary amine-polyoxometalate acid hybrids as asymmetric recoverable iminium-based catalysts

A new strategy for the immobilization of iminium organocatalysts through, the acid-base assembly of multidentate chiral primary amines and solid polyacids is presented, A suitable structurally distinctive C2-symmetric chiral primary amine (CPA)

Development of potent bifunctional endomorphin-2 analogues with mixed μ-/δ-opioid agonist and δ-opioid antagonist properties

The C terminus of endomorphin-2 (EM-2) analogues (Tyr-Pro-Phe-NH-X) was modified with aromatic, heteroaromatic, or aliphatic groups (X = phenethyl,benzyl, phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, tert-butyl, cyclohexyl, or adamantyl; 3-18) to study their effect on opioid activity. Only 9 (1-naphthyl), 11 (5-quinolyl), 16 (cyclohexyl), and 18 (2-adamantyl) exhibited μ-opioid receptor affinity in the nanomolar range (Ki = 2.41-6.59 nM), which, however, was 3-to 10-fold less than the parent peptide. Replacement of Tyr1 by Dmt (2′,6′-dimethyl-L-tyrosine) (19-32) exerted profound effects: (i) acquisition of high μ-opioid receptor affinity (Ki = 0.11-0.52 nM) except 23 (Ph); (ii) presence of potent functional μ-opioid receptor agonism (IC50 1]EM-2), 27 (1-naphthyl), 29 (5-quinolyl), and 32 (5-isolquinolyl); (iii) association of weak δ-opioid antagonist activity (pA2 = 5.41-7.18) except 19 ([Dmt1]EM-2), 20 (H), 27 (1-naphthyl), and in particular 29 (5-quinolyl) with its potent δ-agonism (IC50 = 0.62 nM, pA2 = 5.88); (iv) production of antinociception after ic administration of 32 (5-isoquinolyl) in mice, a bioactivity absent in the corresponding Tyr1 analogue (14); and (v) preferential cis orientation (cis/trans = 3:2 to 7:3) at the Dmt-Pro amide bond, in contrast to the Tyr-Pro amide trans orientation (cis/trans = 1:2 to 1:3). Thus, [Dmt1]EM-2 analogues with hydrophobic C-terminal extensions provide model compounds with potent μ-opioid receptor bioactivity and dual functional agonism.

Synthesis and analgesic activities of urea derivatives of α-amino-N-pyridyl benzene propanamide

New urea L-phenyl alanine derivatives of 4-aminopyridine have been synthesized and evaluated for analgesic activity with the PBQ writhing test in mice and the Randall-Selitto test in rats.Potent oral activity (ID50 10 mg/kg) and good tolerance were foun