126090-32-2

Upstream product

• 103-67-3 benzyl-methyl-amine 
• 67729-36-6 Boc-Phe-O-COO-isoBu 
• 13734-34-4 N-tert-butoxycarbonyl-L-phenylalanine 
• 126090-31-1 N^α-(tert-butoxycarbonyl)-L-phenylalanine-N-benzyl-N-methylamide 

Downstream Products

• 131949-86-5 Boc-Lys(Z)-Phe-NMeBzl 
• 1027266-37-0 {1-[(S)-1-(Benzyl-methyl-carbamoyl)-2-phenyl-ethylcarbamoyl]-1-methyl-ethyl}-carbamic acid tert-butyl ester 
• 131949-71-8 Boc-Asp(OBzl)-Phe-NMe-Bzl 
• 142800-82-6 (N,N-diethylamino)-β-Ala-Thr-D-Trp(CHO)-Phe-NMeBzl 
• 142800-81-5 H-β-Ala-Thr-D-Trp(CHO)-Phe-NMeBzl 
• 126090-13-9 H-Gly-Thr-D-Trp(CHO)-Phe-NMeBzl*0.3AcOH 
• 126090-58-2 Boc-His(Tos)-D-Trp(CHO)-Phe-NMeBzl 
• 126113-10-8 (S)-2-Amino-pentanedioic acid 1-{[(R)-1-[(S)-1-(benzyl-methyl-carbamoyl)-2-phenyl-ethylcarbamoyl]-2-(1-formyl-1H-indol-3-yl)-ethyl]-amide} 5-dimethylamide; hydrochloride 
• 126090-59-3 (S)-2-Amino-N-[(R)-1-[(S)-1-(benzyl-methyl-carbamoyl)-2-phenyl-ethylcarbamoyl]-2-(1-formyl-1H-indol-3-yl)-ethyl]-3-(1H-imidazol-4-yl)-propionamide; hydrochloride 
• 126089-03-0 Boc-Lys(Z)-D-Trp(CHO)-Phe-NMeBzl 
• 126089-05-2 Boc-Orn(Z)-D-Trp(CHO)-Phe-NMeBzl 
• 126089-17-6 Z-β-Ala-Thr-D-Trp(CHO)-Phe-NMeBzl 
• 126089-68-7 Z-Gly-Thr-D-Trp(CHO)-Phe-NMeBzl 
• 126088-90-2 H-Thr-D-Trp(CHO)-Phe-NMeBzl*HCl 

Relevant academic research and scientific papers

Studies of Neurokinin Antagonists. 4. Synthesis and Structure-Activity Relationships of Novel Dipeptide Substance P Antagonists: N2--L-prolyl>-N-methyl-N-(phenylmethyl)-3-(2-naphthyl)-L-alaninamide and Its Related Compounds

As an extension of our studies on discovering a novel substance P (SP) antagonist, we modified the previously reported dipeptide, N2-2-(1H-indol-3-ylcarbonyl)-L-lysyl>-N-methyl-N-(phenylmethyl)-L-phenylalaninamide (2b).The lysine part in 2b was first optimized to a (2S,4R)-hydroxyproline derivative (3h), which is 2-fold more potent than 2b in SP binding assay using guinea pig lung membranes.Next we modified the 1H-indol-3-ylcarbonyl part in 3h.Introduction of a methyl group at the indole nitrogen enhanced the oral activity, while retaining the binding activity.Finally, we modified the phenylalanine part to culminate in the most potent compound 7k (FK888), which is a potent SP antagonist with NK1 selectivity as well as oral activity.

Tetrapeptide Tachykinin Antagonists: Synthesis and Modulation of the Physicochemical and Pharmacological Properties of a New Series of Partially Cyclic Analogs

We report on the synthesis and the pharmacological properties of a new series of tachykinin antagonists based on the pseudopeptide pharmacophore cyclo which contains the 2-azabicyclooctane-3(S)-carboxylic acid (Abo) r

Studies on Neurokinin Antagonists. 2. Design and Structure-Activity Relationships of Novel Tripeptide Substance P Antagonists, Nα-α-(Nα-Acetyl-L-threonyl)-N1-formyl-D-tryptophyl>-N-methyl-N-(phenylmethyl)-L-ph

Continuing studies on the chemical modification of the previously reported novel tripeptide SP antagonist, Nα-α-α-(tert-butyloxycarbonyl)glutaminyl>-N1-formyl-D-tryptophyl>phenylalanine benzyl ester Boc-Gln