849948-75-0

Upstream product

• 100-46-9 benzylamine 
• 7733-29-1 Z-Orn(Boc)-OH 
• 849948-74-9 Fmoc-Orn(Boc)-NHBn 

Downstream Products

• 1408237-88-6 C₂₆H₃₄N₄O₃ 
• 1408237-89-7 (S)-N-benzyl-5-[(tert-butoxycarbonyl)-amino]-2-[((S)-1-cyano-2-phenylethyl)amino]-pentanamide 
• 1408237-87-5 C₃₅H₄₁N₅O₃ 

Relevant academic research and scientific papers

Small molecular PAD4 inhibitor as well as preparation method and application thereof

The invention provides a molecular PAD4 inhibitor as well as a preparation method and application thereof, and belongs to the technical field of biological medicines. Two functional groups are adopted to modify an amino acid skeleton, one functional group is NBD-Cl with the characteristics of low polarity and strong fluorescence, the NBD-Cl is used for modifying the N end of the amino acid skeleton and can be used for subcellular imaging; in addition, due to the fact that the NBD-Cl is small in relative size and lacks reaction orthogonality, interference on the biochemical reaction of organisms is small; the other one is PBA with tumor targeting, the PBA can be combined with a cell membrane by recognizing a cis-diol unit of glycoprotein, the PBA/cis-diol interacts, and a formed dynamic covalent bond can be regulated and controlled by regulating the pH value or adding competitive molecules, so a controllable self-assembly system is realized. The small-molecule PAD4 inhibitor has good oral activity, has an inhibiting effect on tumor growth and metastasis of mice, and also has a treatment effect on arterial thrombosis of rats.

Fluorescence traceable amino acid derivative and preparation method and application thereof

The invention provides a fluorescence traceable amino acid derivative and a preparation method and application thereof, and belongs to the technical field of biological medicines. According to the amino acid derivative provided by the invention, an amino acid skeleton is modified by mainly adopting a functional group capable of realizing fluorescence tracing, the NBD-Cl (4-chloro-7-nitro-2, 1, 3-benzoxaoxadiazole) has the characteristics of low polarity and strong fluorescence, can be used for subcellular imaging by modifying the N end of an amino acid skeleton with the NBD-Cl, and has the advantages of small relative volume, lack of reaction orthogonality and small interference on the biochemical reaction of organisms. Results of the embodiment show that the amino acid derivative capableof being subjected to fluorescence tracing is good in biological activity and can be subjected to fluorescence tracing in vitro and vivo.

Design, synthesis and biological evaluation of new peptide-based ureas and thioureas as potential antagonists of the thrombin receptor PAR1

By applying a diversity oriented synthesis strategy for the search of new antagonists of the thrombin receptor PAR1, a series of peptide-based ureas and thioureas, including analogues of the PAR1 reference antagonist RWJ-58259, has been designed and synthesized. The general synthetic scheme involves reduction of basic amino acid-derived amino nitriles by hydrogen transfer from hydrazine monohydrate in the presence of Raney Ni, followed by reaction with diverse isocyanates and isothiocyanates, and protecting group removal. All new compounds have been evaluated as inhibitors of human platelet aggregation induced by the PAR1 agonist SFLLRN. Some protected peptide-based ureas displayed significant antagonist activity.

A study on the induction of stereoselectivity in the Strecker synthesis of basic amino acid-derived α-amino nitriles

Diverse basic amino acid-derived α-amino nitriles have been synthesized via a modified Strecker reaction, using TMSCN as the cyanide source. It has been found that this synthesis is a slow thermodynamically controlled reaction, where it was difficult to induce stereocontrol. Moderate selectivity was induced by thermodynamic control of the reaction in MeOH. The absolute configuration at the stereogenic center generated was assigned by chemical correlation with 2-oxopiperazine derivatives.

SOMATOSTATIN RECEPTOR 1 AND/OR 4 SELECTIVE AGONISTS AND ANTAGONISTS

The invention relates to (hetero)arylsulfonylamino based peptidomimetics of formula (I), wherein R1, R2, R3, A, B, D, Q, k and n are defined as disclosed, or a pharmaceutically acceptable salt or ester thereof. Compounds of formula (I) possess high affinity and selectivity for the somatostatin receptor subtypes SSTR1 and/or SSTR4 and can be used for the treatment or diagnosis of diseases or conditions wherein an interaction with SSTR1 and/or SSTR4 is indicated to be useful.