22 results about "Phenylalanine derivatives" patented technology

The disclosure relates to double halogenated phenylalanine derivatives, which can be radiolabeled with PET or SPECT radioisotopes, and their use in treating and / or imaging cancer.

The invention discloses a molecular chaperone synergistic blue-copper peptide and application thereof, belongs to the technical field of skin care, and particularly relates to a blue-copper peptide composition formed by compounding blue-copper peptide and N-acetylneuraminic acid, and the structure of the blue-copper peptide is that copper is connected to glycyl-L-histidyl-L-lysine; the blue copper peptide and the N-acetylneuraminic acid are mixed according to the mass ratio of 1: (0.1-1) for use, and further, phenylalanine derivatives can be added into the mixture for compounding. When the blue copper peptide composition obtained by the invention is applied to cells, the cell survival rate is high, the non-enzymatic glycosylation inhibition rate is good, and the expression of Elastin, Col-I and Col-IV mRNA in the cells is high. Therefore, the blue copper peptide composition disclosed by the invention is high in cell survival rate, good in non-enzymatic glycosylation inhibition rate and capable of improving the mRNA expression of Elastin, Col-I and Col-IV in cells, and the application of the blue copper peptide composition.

The present invention provides a small molecule organic piezoelectric material based on phenylalanine derivatives, a preparation method and an application. The preparation method includes the following steps: dissolving an organic small molecule of a phenylalanine derivative in an alcohol solvent to obtain a mixed solution; adding acids of different types and molar ratios to the mixed solution to dope the organic small molecule; and volatilizing the solvent and assembling the organic small molecule to obtain an organic piezoelectric material with different piezoelectric coefficients. The organic small molecule assembly synthesized by the present invention has piezoelectric properties, and the piezoelectric performance can be adjusted by means of acid doping. The preparation method is simple, efficient and environmentally friendly. The piezoelectric device prepared by the method can effectively monitor human movement and can be used in the fields of electronic skin, soft robots, health monitoring, motion monitoring, wearable devices and the like.

The invention provides an on-demand stripping hydrogel with high biological wet tissue adhesion and a preparation method of the on-demand stripping hydrogel. The hydrogel is obtained by combining a hydrophobic amino acid acrylamide derivative and a hydrophilic monomer with a temperature-sensitive monomer and polymerizing. According to the hydrophobic amino acid vinyl monomer phenylalanine derivative provided by the invention, carboxyl and a benzene ring are in a special structure of the same structural unit, so that a hydration layer of a tissue interface can be effectively damaged, and the strength of a matrix can be enhanced by forming stable multiple hydrogen bonds; and strong adhesion (60kPa) can be realized after the adhesive is contacted with wet biological tissues for 5 seconds. The biocompatibility is good, clinical application is facilitated, and a new choice is provided for replacing surgical suture to achieve wound closure and rapid hemostasis clinically.

A method for resolving a phenylalanine derivative of formula (I), and an intermediate. The method comprises: a resolving step comprising using a resolving reagent to react with the phenylalanine derivative represented by formula (I) in a reaction solvent to obtain a resolved intermediate, wherein the resolving reagent is selected from N-acetyl-D-phenylalanine and / or (2R,3R)-(−)-dibenzoyl-L-tartaric acid, and the reaction solvent is selected from 90-99% aqueous ethanol, absolute ethyl alcohol, or acetone. The method uses a chiral reagent to perform salt formation and racemate resolution, and has the advantages of being easy to operate, requiring no special production devices, and being easy to scale up production.

The present invention belongs to the field of pharmaceutical synthesis and specifically discloses an L-phenylalanine derivative tyrosinase inhibitor and its preparation method. The tyrosinase inhibitor comprises a compound represented by formula (I) or a pharmaceutically acceptable salt, ester, stereoisomer, solvate, prodrug, or isotopic variant thereof. The compound represented by formula (I) of the present invention has tyrosinase inhibitory activity superior to that of kojic acid, can inhibit excessive melanin accumulation, and has great application potential in inhibiting mushroom tyrosinase. Therefore, it can be used as a mushroom preservative. The compound represented by formula (I) of the present invention exerts tyrosinase inhibitory activity by acting on amino acid residues and copper ions within the active site and is a reversible competitive inhibitor. #imgabs0#

The invention belongs to the field of medicine synthesis, and particularly discloses an L-phenylalanine derivative tyrosinase inhibitor and a preparation method thereof. The tyrosinase inhibitor comprises a compound shown in a formula (I) or pharmaceutically acceptable salt, ester, stereoisomer, solvate, prodrug or isotope variant thereof. The compound shown in the formula (I) has tyrosinase inhibitory activity superior to that of kojic acid, can play a role in inhibiting excessive accumulation of melanin, and has great application potential in inhibiting mushroom tyrosinase, so that the compound can be used as a mushroom preservative. According to the invention, the compound shown in the formula (I) exerts tyrosinase inhibitory activity through amino acid residues and copper ions acting on active sites, and is a reversible competitive inhibitor. # imgabs0 #

The invention provides a production method of 4-10B-boric acid-L-phenylalanine with high boron atom utilization rate, which comprises the following steps: A, adding strong base and a Turbo Grignard reagent into a 4-halogenated-phenylalanine derivative for reaction, and then adding glycol ester borane for continuous reaction to obtain a 4-boryl-phenylalanine derivative; and B, carrying out acidic hydrolysis on the 4-boryl-phenylalanine derivative, so as to obtain the 4-10B-boric acid-L-phenylalanine. The boron element is introduced into phenylalanine molecules through halogen-metal exchange and electrophilic substitution reaction, wherein the reagent combination of the Turbo Grignard reagent and the glycol ester borane ensures the efficient proceeding of the boronylation process. The production method disclosed by the invention is mild in reaction condition and simple to operate, has high-level comprehensive yield and 10B boron atom utilization rate, and provides a new way for realizing low-cost commercial production of 10B-BPA.

A novel crystalline complex of nicotinamide mononucleotide that is stable and highly safe is provided. The crystalline complex contains nicotinamide mononucleotide and a phenylalanine-based compound. The crystalline complex has L-phenylalanine or aspartame as the phenylalanine-based compound. The crystalline complex having L-phenylalanine as the phenylalanine-based compound has peaks at diffraction angles (2θ) of 19.7±0.2°, 26.4±0.2°, and 32.8±0.2° in a diffraction pattern of powder X-ray diffraction measured with a Cu-Kα ray as an X-ray source. The crystalline complex having aspartame as the phenylalanine-based compound has peaks at diffraction angles (2θ) of 7.0±0.2°, 10.7±0.2°, 14.4±0.2°, and 29.1±0.2° in a diffraction pattern of powder X-ray diffraction measured with a Cu-Kα ray as an X-ray source.

The present application relates to a kind of containing effective amount of novel acyl phenylalanine derivative of general formula (I), its preparation method and the use of the derivative as a pharmaceutical composition as a drug, compared with prior art, with more broad application prospect.

The invention discloses a compound, a composite material, a thin film and a photoelectric device containing the compound, the compound is a phenylalanine derivative, the compound comprises an amide group and an aromatic group, a metal oxide material can be modified and treated, the surface defect state of the metal oxide material can be effectively passivated, the agglomeration phenomenon is improved, and the photoelectric device has the advantages that the photoelectric device is stable in performance; and the amide group in the compound can form a hydrogen bond with the hydroxyl group on the surface of the metal oxide material, so that the negative influence of the compound on the conductivity of the metal oxide material is reduced or eliminated.

The invention discloses a method for activating an aryl chloride C (sp2)-Cl bond to generate an aryl phenol compound, which is characterized in that a visible light excitation photosensitizer is utilized for catalysis, and in a reaction solvent, a raw material in a formula (1) realizes C (sp2)-Cl bond breakage to generate the aryl phenol compound in a formula (3) under the auxiliary catalysis condition of acid. Under the conditions of room temperature and normal pressure, water is used as an oxygen source, so that the method is green and environment-friendly, the reaction operation is simple, the substrate universality is wide, the functional group tolerance is good, and the reaction yield is high; the reaction not only can realize simple aryl chloride conversion, but also can realize conversion of various amino acid derivatives and drug molecules such as phenylalanine derivatives, ketoprofen derivatives, biphenyl derivatives, bupropion, clofibrate, pyrimethamine and the like to generate corresponding aryl phenol compounds; and compared with the common tubular reaction, the fluid amplification efficiency is improved by nearly hundreds of times. The invention provides a new thought and method for synthesis of the aryl phenol compound, and has a wide application prospect.

The invention discloses application of a triple hydrocarbon activation strategy to synthesis of novel fluorescent amino acid, belonging to the technical field of organic synthesis. The method comprises the following steps: by taking phenylalanine derivatives and diaryl acetylene as starting substrates, reacting for 12 hours at the temperature of 120 DEG C under the action of a rhodium catalyst to obtain a series of five-fused-ring fluorescent amino acids. The method has the advantages that raw materials are easy to prepare, only one reaction step is needed, and experimental operation is simple; fluorescence experiments show that the obtained fluorescent amino acid has good fluorescence, and the maximum emission wavelength is as high as 628nm; a cell co-localization experiment shows that the five-ring-fused fluorescent amino acid has a good targeting effect on cell lysosome. # imgabs0 #

The present invention discloses a copper peptide composition and its application, belonging to the technical field of skin care. Specifically, it relates to a copper peptide composition composed of a copper peptide and N-acetylneuraminic acid. The structure of the copper peptide is that copper is linked to glycyl-L-histidyl-L-lysine. The copper peptide and N-acetylneuraminic acid are mixed and used in a mass ratio of 1:0.1-1. Further, phenylalanine derivatives can be added for compounding. When the obtained copper peptide composition of the present invention is applied to cells, the cell survival rate is high, the non-enzymatic glycosylation inhibition rate is good, and the expressions of Elastin, Col-I, and Col-IV mRNA in the cells are high. Therefore, the present invention is a copper peptide composition with a high cell survival rate, a good non-enzymatic glycosylation inhibition rate, and an improvement in the expressions of Elastin, Col-I, and Col-IV mRNA in cells, and its application.

The application discloses a phenylalanine derivative small molecule self-assembly body with piezoelectric performance, a preparation method and application thereof, relates to the technical field of functional materials, and through introduction of a chiral solvent complementary to the configuration of the phenylalanine derivative small molecule and combination of reverse-solvent water synergistic regulation, the solution polarity is significantly changed, the small molecule solubility is reduced, the molecule is promoted to quickly and directionally nucleate and self-assemble, a highly ordered microstructure is formed, molecular-level chiral space control is realized, and the piezoelectric performance is improved. The piezoelectric material can be widely applied to the fields of flexible sensors, biomedical devices, energy collection devices and the like.

The invention provides a pharmaceutical composition for promoting pancreatic beta cell proliferation. The pharmaceutical composition comprises a compound shown in a formula I or a stereoisomer, a hydrate, a solvate, an isotope label, a prodrug or a pharmaceutically acceptable salt and a pharmaceutically acceptable carrier of the compound. The invention also provides a compound as shown in a formula I or a stereoisomer, a hydrate, a solvate, an isotope label, a prodrug or a pharmaceutically acceptable salt of the compound or a pharmaceutically acceptable salt containing the compound as shown in the formula I or the stereoisomer, the hydrate, the solvate and the isotope label of the compound. The invention also discloses application of a pharmaceutical composition of the prodrug or pharmaceutically acceptable salt thereof in preparation of drugs for promoting pancreatic beta cell proliferation. # imgabs0 #

The disclosure relates to double halogenated phenylalanine derivatives, which can be radiolabeled with PET or SPECT radioisotopes, and their use in treating and / or imaging cancer.

The invention provides a bioactive nanogel coating on the surface of an intravascular stent as well as a preparation method and application of the bioactive nanogel coating. The coating is formed by blending a D-type phenylalanine derivative gel factor and a terminal REDV modified D-type phenylalanine derivative gel factor and can be self-assembled to form a stable nano spiral fiber-shaped gel coating structure, the unique extracellular matrix imitating structure and REDV can play a synergistic biological role, related protein adsorption is effectively regulated and controlled, and the application range is wide. Adhesion and proliferation of smooth muscle cells are remarkably inhibited; meanwhile, migration, adhesion and proliferation of vascular endothelial cells are selectively promoted, rapid re-endothelialization of the stent is achieved, and inflammation, thrombus, intimal hyperplasia and restenosis are inhibited. The component structure of the coating is bionic, the biocompatibility is excellent, the interface bonding force with a stent base body is good, the biological activity and effectiveness can be remarkably improved, the implantation degradation behavior of the degradable metal stent can be effectively regulated and controlled, and the biological safety is improved. Meanwhile, the preparation method of the coating is simple, convenient and feasible, and has a clinical transformation application prospect.

The invention discloses phenylalanine ammonia mutase and application of the phenylalanine ammonia mutase in preparation of R-type beta-amino acid. Compared with an amino acid sequence as shown in SEQ ID NO: 1, the amino acid sequence of the phenylalanine ammonia mutase comprises the amino acid residue difference of one or more of the following sites: the 59th site, the 60th site, the 144th site, the 233th site, the 247th site, the 281th site, the 304th site, the 330th site, the 394th site, the 396th site, the 399th site, the 403th site and the 427th site. The (R)-beta-phenylalanine derivative is synthesized by adopting the enzyme, so that the regioselectivity, enantiomer selectivity and conversion rate of the product can be obviously improved.

The disclosure relates to double halogenated phenylalanine derivatives, which can be radiolabeled with PET or SPECT radioisotopes, and their use in treating and / or imaging cancer.

The present invention relates to a photoisomerizable chiral hydrogel material, its preparation method, and application, belonging to the field of supramolecular materials. The photoisomerizable chiral hydrogel material is synthesized by modifying a symmetrical phenylalanine derivative with a stilbene derivative through a three-step liquid-phase reaction (amidation, trifluoroacetic acid deprotection, and amidation). The structural formula of the hydrogel material is shown as (I) or (II). The chirally uniform nanogel material prepared by the present invention successfully mimics the chiral helical structure of the extracellular microenvironment. The preparation method is simple, and the resulting hydrogel has excellent biocompatibility and can achieve damage-free three-dimensional encapsulation and photocontrolled release of cells. It has promising application prospects in fields such as controlled-release drug carriers and tissue engineering scaffold materials.

The present invention relates to a recombinant cell. The recombinant cell may express a first enzyme, a second enzyme and a third enzyme and produce a nonstandard amino acid (nsAA). The first enzyme may be a L-threonine transaldolase (L-TTA) or a threonine aldolase (TAs). The second enzyme may be a phenylserine dehydratase or a threonine deaminase (TD). The third enzyme may be an aminotransferase (AT), a L-amino acid dehydrogenase (L-AADH) or a D-amino acid aminotransferase. At least one of the first enzyme, the second enzyme and the third enzyme may be heterologous to the recombinant cell. Also provided are a method for producing a nonstandard amino acid (nsAA) by the recombinant cell and a method for producing a nsAA in a container in the presence of the first enzyme, the second enzyme and the third enzyme.