212567-95-8

Upstream product

• 152120-54-2 N,N'-bis( tert-butoxycarbonyl)-1H-pyrazole-1-carboxamidine 
• 660-88-8 5-aminopentanoic acid 
• 170983-44-5 tert-butyl N-[[tert-butoxycarbonylamino]-[5-hydroxypentylamino]methylene]carbamate 
• 2508-29-4 5-hydroxypentylamine 

Downstream Products

• 936571-58-3 N,N'-bis-tert-butoxycarbonyl-4-(5-guanidino-pentanoylamino)-benzoic acid methyl ester 
• 936571-61-8 C₃₃H₄₆N₄O₇ 
• 1032374-60-9 C₂₉H₄₄N₄O₉ 
• 936571-59-4 4-{tert-butoxycarbonylmethyl-[5-(N,N'-bis-tert-butoxycarbonyl)guanidino-pentanoyl]amino}-benzoic acid methyl ester 
• 1032374-61-0 C₂₉H₄₅N₅O₈ 
• 936571-60-7 4-{(tert-butoxycarbamoyl-methyl)-[5-(N,N'-bis-tert-butoxycarbonyl)guanidino-pentanoyl]amino}-benzoic acid methyl ester 
• 1032374-62-1 C₃₂H₄₄N₄O₇ 
• 936571-76-5 2(S)-(2(S)-{4-[carboxymethyl-(5-guanidino-pentanoyl)-amino]benzoylamino}-3-methyl-butyrylamino)-3-phenyl-propionic acid 
• 936571-78-7 2(S)-(2(S)-{4-[(5-guanidino-pentanoyl)-(3-phenyl-propyl)-amino]-benzoylamino}-3-methyl-butyrylamino)-3-phenyl-propionic acid 
• 936571-77-6 2(S)-(2(S)-{4-[(tert-butylcarbamoyl-methyl)-(5-guanidino-pentanoyl)-amino]benzoylamino}-3-methyl-butyrylamino)-3-phenyl-propionic acid 
• 1206479-83-5 C₃₅H₄₈F₆N₁₂O₅ 
• 1206480-16-1 C₅₆H₇₄N₈O₁₄S 
• 1206480-28-5 C₈₂H₁₂₂F₆N₁₄O₂₂S₂ 
• 1224096-03-0 C₇₀H₉₈F₆N₁₄O₁₈ 

Relevant academic research and scientific papers

INTEGRIN TARGETING LIGANDS AND USES THEREOF

Synthetic ανβ6 integrin ligands of Formula (I) having serum stability and affinity for integrin ανβ6, which is a receptor expressed in a variety of cell types, are described. The described ligands are usful for delivering cargo molecules, such as RNAi agents or other oligonucleotide-based compounds, to cells that express integrin ανβ6, and thereby facilitating the uptake of the cargo molecules into these cells. Compositions that include ανβ6 integrin ligands and methods of use are also described Formula (I).

Exploratory studies on soluble small molecule CD4 mimics as HIV entry inhibitors

Several small molecule CD4 mimics, which inhibit the interaction of gp120 with CD4, have been developed. Original CD4 mimics such as NBD-556, which has an aromatic ring, an oxalamide linker and a piperidine moiety, possess significant anti-HIV activity bu

Preparation method and application of diosgenin derivative and DHA self-assembled nanoparticles

The invention discloses a preparation method and application of diosgenin derivative and DHA self-assembled nanoparticles. The preparation method comprises the following steps of: taking a proper amount of diosgenin to react with Boc-pentylamino 5-acid, removing Boc to form an intermediate, and further reacting and purifying to obtain DGG; weighing 1.9 mg of DGG and dissolving it in 335 [mu] L of CH3OH, and carrying out ultrasonic dissolution; dissolving 0.4 mg of DHA in 50 [mu] L of CH3OH, mixing the two solutions, carrying out uniform ultrasonic dissolution to obtain a mixed solution, dispersing the mixed solution into 750 [mu] L of water at a stirring speed of 500 r/min and a speed of 15 s/drop, stirring at a speed of 500 r/min for 3 h to obtain the DGG/DHA-HA self-assembled nanoparticles, and carrying out surface modification with HA to obtain the DGG/DHA-HA self-assembled nanoparticles (DGG/DHA-HA NPs). According to the self-assembled nanoparticles prepared by the invention, the synergistic anti-tumor activity and nerve protection effect can be remarkably improved, and the problems of solubility, stability and the like of DGG and DHA can be remarkably improved.

Synthesis and structure-activity relationships of small-molecular di-basic esters, amides and carbamates as flaviviral protease inhibitors

Inhibitors of the flaviviral serine proteases, which are crucial for the replication of dengue and West-Nile virus, have attracted much attention over the last years. A dibasic 4-guanidinobenzoate was previously reported as inhibitor of the dengue protease with potency in the low-micromolar range. In the present study, this lead structure was modified with the intent to explore structure-activity relationships and obtain compounds with increased drug-likeness. Substitutions of the guanidine moieties, the aromatic rings, and the ester with other functionalities were evaluated. All changes were accompanied by a loss of inhibition, indicating that the 4-guanidinobenzoate scaffold is an essential element of this compound class. Further experiments indicate that the target recognition of the compounds involves the reversible formation of a covalent adduct.

NO-RELEASING GUANIDINE-COXIB ANTI-CANCER AGENTS

The present disclosure provides NO-releasing guanidine-coxib anti-cancer agents, having the structure of Formula (I): wherein R1, R11, Z and L are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds of Formula (I); and methods useful for healing wounds, preventing and treating cancer, or treating actinic keratosis, cystic fibrosis, acne, or a disease mediated by arginine deficiency using a compound of Formula (I)

Modifications of the GSK3β substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics

Amplification, overexpression, and elevated activation of Akt have been detected in many human malignancies making it an important target for cancer therapy. The Akt substrate-binding site offers a large number of potential interactions to an appropriatel

Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone

Inhibitors of human mast cell tryptase (EC 3.4.21.59) have therapeutic potential for treating allergic or inflammatory disorders. We have investigated transition-state mimetics possessing a heterocycle-activated ketone group and identified in particular benzothiazole ketone (2S)-6 (RWJ-56423) as a potent, reversible, low-molecular-weight tryptase inhibitor with a Ki value of 10 nM. A single-crystal X-ray analysis of the sulfate salt of (2S)-6 confirmed the stereochemistry. Analogues 12 and 15-17 are also potent tryptase inhibitors. Although RWJ-56423 potently inhibits trypsin (Ki = 8.1 nM), it is selective vs other serine proteases, such as kallikrein, plasmin, and thrombin. We obtained an X-ray structure of (2S)-6 complexed with bovine trypsin (1.9-? resolution), which depicts inter alia a hemiketal involving Ser-189, and hydrogen bonds with His-57 and Gln-192. Aerosol administration of 6 (2R,2S; RWJ-58643) to allergic sheep effectively antagonized antigen-induced asthmatic responses, with 70-75% blockade of the early response and complete ablation of the late response and airway hyperresponsiveness.

PEPTIDE DERIVATIVES AND MEDICINAL COMPOSITIONS

An object of the present invention is to provide a novel nociceptin receptor agonist. The present invention relates to a peptide derivative represented by the following general formula (1): ???(in which A represents alkylene, -(CH2)nCO- or a group represented by the following formula (2) or (3): wherein n represents an integer of 1 to 8; X and Y are same or different and each represents -CONH- or -CH2NH-; R1, R2 and R3 are same or different and each represents alkyl, aryl or heteroaryl; Z represents -CON(R4)R5 or -CH2N(R4)R5; and R4 and R5 are same or different and each represents hydrogen, alkyl, aryl or heteroaryl) or a pharmaceutically acceptable salt thereof. A pharmaceutical composition according to the present invention is useful as a nociceptin receptor agonist.