113 results about "Macrocyclic lactone" patented technology

According to the scheme, the invention provides the recombinant macrolide enzyme as well as the preparation method and the application thereof, the amino acid sequence of the recombinant macrolide enzyme is as shown in SEQ ID NO.1, and the recombinant macrolide enzyme is derived from an EreC esterase family of enterobacter hormaechei and is obtained through site-specific mutagenesis; the mutation sites are as follows: glutamic acid at the 44th site is mutated into asparagine, tyrosine at the 55th site is mutated into proline, proline at the 76th site is mutated into arginine, phenylalanine at the 153rd site is mutated into alanine, and serine at the 219th site is mutated into glutamic acid. The method is expected to remove macrolide antibiotic pollution, and has good economic benefits and practical values.

The present invention provides a method for enhancing the removal of resistance genes and promoting humification in aerobic composting. The method comprises the following steps: mixing livestock and poultry manure with a composting auxiliary material, adjusting the moisture content to 55%-65%, and adding a MnFe2O4 additive to obtain a composting raw material; aerobically composting the material, turning the compost every 2-3 days during a temperature rise period and a high temperature period, and every 7 days during a temperature fall period and a mature period, with the aerobic composting time being 20-30 days. Compared with a conventional composting method, the relative abundances of sulfonamide, tetracycline, macrolide, and aminoglycoside resistance genes in the mature compost obtained by the method are reduced by 60%-73%, 50%-57%, 20%-80%, and 45%-66%, respectively, and the humic acid (HA) content is increased by about 15%. Meanwhile, the method achieves efficient harmlessness and resource utilization of organic solid waste, and has the potential for large-scale production.

A method for enhancing resistance gene removal and promoting humification in an aerobic compost, which method comprises mixing livestock and poultry manure with compost auxiliary materials, adjusting the water content, adding an MnFe2O4 additive, and then performing aerobic composting for 20-30 days. Compared with conventional composting methods, the mature compost product obtained by means of the method exhibits a 60%-73% reduction in the relative abundance of sulfonamide resistance genes, a 50%-57% reduction in tetracycline resistance genes, a 20%-80% reduction in macrolide resistance genes, and a 45%-66% reduction in aminoglycoside resistance genes, and shows approximately a 15% increase in humic acid HA. This method achieves both efficient harmless treatment and resource utilization of organic solid waste.

The invention provides a compound as shown in a formula (I), and a stereoisomer, a tautomer, an isotope label, nitrogen oxide, a solvate, a polymorphic substance, a metabolite, ester, pharmaceutically acceptable salt or prodrug thereof, or a pharmaceutical composition thereof, which have better antibacterial and anti-inflammatory effects, can be used as an antibiotic, and can be used for preparing a pharmaceutical preparation for preventing and treating diseases. The compound can treat infection caused by pathogenic microorganisms resistant to erythromycin and telithromycin, and simultaneously acts on double targets of ribosome and topoisomerase.

The invention belongs to the technical field of microbial pharmacy, and discloses a polyketone macrolide compound generated by genetically engineered streptomyces as well as a preparation method and application thereof. The polyketone macrolide compound disclosed by the invention is a cinnamyl streptomycin derivative, has cell proliferation inhibition activity better than that of a natural product Cinnamomycin A-D, can exert anti-tumor activity by inhibiting activity of human exonucleotide pyrophosphatase / phosphodiesterase 1 (ENPP1) and activating an inherent immune pathway, can be prepared into a medicine or a medicinal composition, and can be used for preparing medicines or medicinal compositions. The compound is used for treating tumors and related diseases.

The present application relates to the field of polymer chemistry and biomedical technology, and particularly relates to a macrocyclic lactone polymer shown in formula (I) which is used for preventing or treating hyperproliferative diseases, including liver cancer, leukemia, breast cancer, colon adenocarcinoma, gastric cancer, lung cancer, Barrett's esophageal cancer, cervical cancer, pancreatic cancer, endometrial cancer, bone cancer, lymphoma, kidney cancer, brain cancer, nerve cancer, nasopharyngeal cancer, oral cancer, bladder cancer, colorectal cancer and melanoma, and has the potential to be developed into a new type of antitumor drug.

The invention describes an extended-release composition comprising PLGA or PLA polymeric microspheres comprising an isoxazoline, preferably sarolaner, and a macrocyclic lactone, preferably moxidectin, and wherein the composition further comprises at least one pharmaceutically acceptable excipient; and uses thereof.

The present invention relates to a pyrazine macrolide compound and the use thereof. Specifically disclosed is a compound as represented by formula I or a pharmaceutically acceptable salt thereof. The compound of the present invention exhibits activity against bacteria, mycoplasmas, or chlamydias, and is useful for preventing and / or treating diseases caused by bacteria, mycoplasmas, or chlamydias. Further, the compound of the present application can achieve an antibacterial activity comparable to or better than that of azithromycin or solithromycin at a lower dosage. Furthermore, the compound of the present application achieves a superior antibacterial effect on Gram-positive bacteria. Still furthermore, the compound of the present application exhibits a better inhibitory activity against mycoplasmas and a lower hepatotoxicity.

The invention relates to a novel 16-membered macrolide compound 13alpha-O-alpha-L-oleandrosyl-23-alpha-hydroxy-25-isopropyl milbemycin beta3, a preparation method of the novel 16-membered macrolide compound 13alpha-O-alpha-L-oleandrosyl-23-alpha-hydroxy-25-isopropyl milbemycin beta3, and an application of the novel 16-membered macrolide compound 13alpha-O-alpha-L-oleandrosyl-23-alpha-hydroxy-25-isopropyl milbemycin

The ester derivatives of brefeldin A represented by Formula (I) in the inhibition of tumor proliferation. The compounds are prominent in the prevention or treatment of hyperproliferative diseases, including liver cancer, leukemia, breast cancer, colon adenocarcinoma, gastric cancer, lung cancer, Bart's esophageal cancer, cervical cancer, pancreatic cancer, endometrial cancer, bone cancer, lymphoma, kidney cancer, brain cancer, nerve cancer, nasopharyngeal cancer, oral cancer and colorectal cancer, and have the potential to be developed as antitumor agents.

The invention belongs to the field of medicines, and relates to a macrolide derivative as well as a preparation method and application thereof. The macrolide derivative is a compound as shown in a structural general formula (I), a salt thereof or an optical isomer thereof: (I), wherein R1 is selected from NR8R9, a C3-C8 nitrogen-containing aliphatic ring and a substituted C3-C8 nitrogen-containing aliphatic ring. The macrolide derivative disclosed by the invention has better chemical stability than 17-glucoside spinosad, and has a better tumor inhibition effect in a human body environment, so that the macrolide derivative is expected to be used as an anti-tumor potential drug.

The invention discloses a method for preparing an ester compound and a macrolide compound, and belongs to the technical field of organic chemistry, the preparation method of the ester compound is as follows: in an organic solvent, an alpha-carbonyl alkenyl ester compound reacts with alcohol or phenol under the catalytic condition of alkali to obtain the ester compound; the preparation method of the macrolide compound comprises the following step: in an organic solvent, carrying out intramolecular hydroxyl reaction on an alpha-carbonyl alkenyl ester compound under the catalysis condition of alkali or acid, thereby obtaining the macrolide compound. The method is wide in substrate range, high in practicability and high in yield, racemization of a carboxylic acid alpha-chiral center can be inhibited in intermolecular esterification reaction and macrocyclic lactonization reaction, and the method can be applied to total synthesis of a Brevicidine natural product containing a 13-membered cyclic ester peptide core structure; the method disclosed by the invention has the advantages of mild reaction conditions, simplicity, easiness in operation, wide substrate adaptability, no racemization of the product and the like.

The present invention provides an anti-parasitic composition for use in the treatment or prevention of a parasitic infection in a mammal, the anti-parasitic composition comprising a macrolide, in particular a combination of ivermectin, abamectin and doramectin. The invention also provides a method of treating a parasitic infection in a mammal by administering to the mammal an effective amount of an anti-parasitic composition comprising ivermectin, abamectin, and doramectin, and a method of preparing the anti-parasitic composition.

According to the scheme, the recombinant macrolide enzyme and the preparation method and application thereof are provided, the amino acid sequence of the recombinant macrolide enzyme is shown as SEQ ID NO.1, and the recombinant macrolide enzyme is obtained by site-directed mutagenesis of an erythromycin esterase family protein sequence derived from enterobacter hormaechei; the mutation sites are as follows: the 44 glutamic acid is mutated into asparagine, the 55 tyrosine is mutated into proline, the 153 proline is mutated into alanine, and the 219 serine is mutated into glutamic acid, so that the specific macrolide lactonase which is efficient, stable, easy to prepare on a large scale and more suitable for environmental requirements is prepared, and macrolide antibiotic pollution is removed; and the method has good economic benefits and practical values.

The invention discloses a novel Fe-C-N-coated Au material and a preparation method and application thereof.According to the Fe-C-N-coated Au material, iron monatomic nano-enzyme Fe-C-N serves as a core, gold nanoparticles are loaded on the surface, the Fe-C-N nanoparticles and a HAuCl4 aqueous solution are stirred at low temperature, then an ice-cold NaBH4 solution is slowly added into a mixed solution, and the Fe-C-N-coated Au material is obtained after reaction and treatment. The novel Fe-C-N-coated Au material disclosed by the invention can be used for rapidly and sensitively detecting the azithromycin or macrolide drug-resistant gene ermB.

The application provides a macrolide derivative and a preparation method and application thereof, relates to the technical field of medicinal chemistry, and the macrolide derivative is a compound with a general structure shown in the following formula I: in the formula, A is selected from any one of alkynyl, alkenyl or piperazine; R is selected from any one of H or F; X is selected from any one of CH or N, Y is selected from any one of methyl, ethyl or cyclopropyl, and n is an integer in the range of 2-6. The macrolide derivative is connected by different lengths of ether hydrocarbons at the 3-position, thereby avoiding the problem that the instability of a synthesized compound is caused by using an ester group as a side chain to connect a quinolone group. The application successfully prepares a macrolide derivative with double targets, and the antibacterial activity of the macrolide derivative is obviously better than the antibacterial activity of erythromycin, telithromycin, clarithromycin and ciprofloxacin which only have single targets.

Provided are 13-membered macrolides for the treatment of infectious diseases. The 13-membered macrolides described herein are azaketolides. Also provided are methods for preparing the 13-membered macrolides, pharmaceutical compositions comprising the 13-membered macrolides, and methods of treating infectious diseases, and in particular, disease resulting from Gram negative bacteria using the disclosed macrolides. Formula (I)

The application discloses a preparation method and application of a cobalt monatomic doped strontium titanate composite material, and belongs to the field of water treatment. The cobalt doped strontium titanate composite catalytic material is composed of a cobalt metal doped strontium titanate material. A preparation process uses tetrabutyl titanate and a nitrate as reactants, ethylene glycol and water as solvents, and prepares strontium titanate (SrTiO3: STO) through a hydrothermal method. Then, cobalt monatomic atoms are doped into the strontium titanate through cobalt chloride (a cobalt source) by using an electrostatic adsorption method, so as to form cobalt doped strontium titanate (Co-STO). The material can efficiently activate an oxidant peracetic acid and rapidly degrade various antibiotic pollutants, and especially performs well in degrading quinolone, tetracycline and macrolide antibiotics. The catalytic material has the advantages of low cost, renewability and environmental protection, and is very suitable for being applied to a deep treatment process of pharmaceutical wastewater.

The invention relates to a method for analyzing pollutants in hospital wastewater based on liquid chromatography-high resolution mass spectrometry. The method comprises the following steps: S1, enriching pollutants in hospital wastewater through solid-phase extraction of four specific solid-phase extraction columns, and then analyzing and detecting a liquid to be detected through a specific chromatographic column, a specific liquid chromatography and a high-resolution mass spectrometry which are connected in series; the identification of various pollutants (medicines and metabolites thereof) in the hospital wastewater is realized, so that a data basis is provided for subsequent fingerprint analysis. Specifically, the analysis method provided by the invention can identify 34 kinds of substances, including sulfonamide antibiotics, macrolide antibiotics, cephalosporin antibiotics, quinolone antibiotics, beta-lactam antibiotics, aminoglycoside antibiotics and carbamazepine and metabolites thereof.

The disclosure provides a polyene. The polyene comprises two sugar moieties and / or is modified in an exocyclic carboxylic acid position, or is a pharmaceutically acceptable salt, solvate, tautomeric form or polymorphic form thereof. In some embodiments, the polyene is a compound of formula I. The disclosure extends to pharmaceutical and agrochemical compositions, preservatives and foodstuffs comprising the polyene. The disclosure also extends to the polyene or pharmaceutical composition for use as a medicament, for use in treating, preventing or ameliorating an infection or a prion disease and methods of treating a disease in a plant or a mushroom using the polyene. The disclosure further provides a method of producing a polyene comprising a sugar moiety and / or a modification at an exocyclic carboxylic acid thereon. Finally, the disclosure also extends to a recombinant organism or cell expressing a glycosyltransferase enzyme or an amidotransferase enzyme.

To provide a technique relating to total secretion regulation of sebaceous gland cells.SOLUTION: The present invention provides a total secretion regulator comprising a compound selected from the group consisting of oligosaccharides and macrolide compounds as an active ingredient.SELECTED DRAWING: None

We report improved adjuvant compounds that have an aryl 2-aminoimidazole structure for macrolide potentiation against a virulent strain of gram-negative bacteria, AB5075. Compounds were discovered to retain significant adjuvant activity at 10 μM, lowering the minimum inhibitory concentration (MIC) of clarithromycin (CLR) from 8-fold to 128-fold or greater. 2-Aminoimidazole compounds linked to aryl groups via either an amide or urea linker showed significantly improved activity over control compounds.

The application relates to a kind of macrolide polymers and its preparation method and the application of inhibiting the effect of proinflammatory cytokines, and is related to the field of polymer chemistry and biomedical technology, specifically to the application of a kind of macrolide derivative shown in formula (I) in the preparation of proinflammatory cytokine effect inhibitor drugs, which has the potential to be developed as a new type of inflammation factor activity inhibitor drug.

This invention discloses a method for synthesizing lactone compounds and cerium-catalyzed lactone compounds. The synthesis method comprises the following steps: under visible light irradiation, in an oxygen atmosphere, and in the presence of a photocatalyst and a cerium catalyst, a cyclic ketone compound containing a structural fragment as shown in Formula II is subjected to a cyclization reaction in a solvent to obtain a lactone compound containing a structural fragment as shown in Formula I. This method uses readily available raw materials to conveniently and rapidly synthesize various medium- and large-cyclic lactones, and is simple, economical, and environmentally friendly.

Provided herein are synthetic methods and intermediates useful in the preparation of polyketides, including 12-membered ring macrolides. These synthetic methods and intermediates provide scalable access to polyketides, including polyketides with potent bioactive splicing modulator activity and therapeutic potential, including treating various types of cancer. The polyketides include 12-membered ring macrolides, including Compound A, Compound B, and pladienolides, including pladienolide A, pladienolide B, pladienolide C, pladienolide D, pladienolide E, pladienolide F, and pladienolide G.

The invention discloses a macrolide and isoxazoline medicine combined local external preparation for dogs as well as a preparation method and application thereof, belongs to the technical field of veterinary medicines, and solves the problems that an existing preparation is limited in solvent selection, lacks a long-acting slow-release mechanism, is relatively high in medicine release speed, cannot maintain an effective concentration on the body surface of a dog for a long time, and cannot be used for a long time. The local external preparation is prepared from the following raw materials: a preparation main material, an auxiliary solvent, a synergist, a transdermal penetration enhancer, an antioxidant and a surface film-forming agent, according to the macrolide and isoxazoline medicine combined local external preparation for dogs, the solvent, the synergist and the transdermal penetration enhancer with good solubility are selected for combined use in preparation of the preparation, so that the medicine can be effectively dissolved, the permeability of the medicine in the skin of dogs is improved, the purpose of long-acting medicine release is achieved, and the curative effect of the dogs is improved. The bioavailability of the medicine is improved.

A new class of dimeric 2-aminoimidazole (2-AI) compounds that potentiate macrolide antibiotics against A. baumannii. A parent dimer lowers the MIC of clarithromycin (CLR) from 32 μg / mL to 1 μg / mL at a concentration of 7.5 μM (3.4 μg / mL), while a structure activity relationship (SAR) study on the dimeric 2-AI scaffold resulted in the identification of several compounds with increased activity. Substitution of fluorine on a central phenyl ring resulted in the most potent activity, with the lead compound, containing a fluorine ortho to each of the 2-AIs, that lowered the CLR MIC to 2 μg / mL against AB5075 at 1.5 μM (0.72 μg / mL), exceeding the activity of both the parent dimer and the lead aryl-2-AI. Furthermore, these dimeric 2-AI analogs exhibit favorably low mammalian cell toxicity.

The invention relates to the field of medicines, in particular to a hydroxypyridone coupled macrolide compound shown in a formula (I) or a formula (II) and application of the hydroxypyridone coupled macrolide compound in preparation of an antibacterial agent and a bacterial biofilm inhibitor. In-vivo and in-vitro pharmacological verification shows that most of the hydroxypyridone coupled macrolide compounds have antibacterial activity, can be used for preparing antibacterial agents and anti-biofilm agents, and have the potential of being developed into novel antibacterial drugs.