63 results about "Macrocyclic lactone" patented technology

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 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 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 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)

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.

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.

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.

This article provides a macrolide-quinolone compound of formula (I) which has good antibacterial and anti-inflammatory effects and can be used as an antibiotic, especially for the treatment of infections caused by erythromycin-resistant pathogens in clinical practice.

This invention relates to the field of agricultural biological control technology, specifically disclosing a novel bafilomycin analogue with antifungal activity, its preparation method, and its application. The bafilomycin analogue is a novel natural compound obtained by fermentation culture of Streptomyces sp. TH21, component activity tracing, and subsequent separation and extraction. This type of compound exhibits good activity against plant pathogenic fungi and has the potential to be developed into a novel, highly efficient, and environmentally friendly biological fungicide.

The present invention relates to methods for converting unsaturated macrocyclic ketones to lactones wherein the conversion is catalyzed by a Baeyer-Villiger monooxygenase (BVMO). The invention also relates to the use of a Baeyer-Villiger monooxygenase for the conversion of unsaturated macrocyclic ketones to lactones and provides certain novel macrocyclic lactones, which are accessible by the method according to the invention. Furthermore, the present invention relates to the use of novel and known macrocyclic lactones as fragrances.

The application discloses a synergistic bactericidal composition, comprising the following components: a toona sinensis extract: 16-2048 mu g / mL; a macrolide antibiotic: 0.0625-4096 mu g / mL; the bacteria are staphylococcus aureus or methicillin-resistant staphylococcus aureus, and the macrolide antibiotic is erythromycin or azithromycin. The application further discloses a use of the synergistic bactericidal composition in preparation of a medicine for treating skin and soft tissue infections. The composition provided by the application can convert the traditional macrolide antibiotics such as erythromycin and azithromycin which only have a bacteriostatic effect into a preparation which has clear bactericidal activity on staphylococcus aureus and drug-resistant strains thereof. After the toona sinensis extract is combined with the antibiotic, a synergistic effect is exhibited, and the concentration of the toona sinensis extract and the antibiotic required when the toona sinensis extract and the antibiotic are used alone can be greatly reduced.

The invention relates to a molecular marker of drug-resistant mycobacterium abscessus based on fusA gene mutation and application of the molecular marker, and belongs to the technical field of biological medicines. The invention provides a group of molecular markers for detecting the drug resistance of mycobacterium abscessus. The molecular markers are mutations on a fusA gene of the mycobacterium abscessus, including fusA1318Agt; g, fusA 1613 G gt; a, fusA18721883 dup GGGCGACGTGAT, and the number of the GGGCGACGTGAT is 1: 1. The invention finds that when the mycobacterium abscessus generates fusA1613 G gt; when A is mutated, cross resistance is generated to aminoglycoside drugs, macrolide drugs and tetracycline drug tigecycline. The fusA < 1318 > A < gt > is generated; the mycobacterium abscessus with mutations of G and fusA18721883 dup GGGCGACGTGAT is resistant to aminoglycoside drugs and tigecycline, and meanwhile, the mycobacterium abscessus has lateral sensitivity to macrolide drugs. The mycobacterium abscessus with mutations of G and fusA18721883 dup GGGCGACGTGAT is resistant to aminoglycoside drugs and tigecycline. The method is of great significance to clinical molecular diagnosis and medication.

This invention discloses a screening and detection method for antibiotic residues in organic fertilizers, relating to the field of trace residue detection. The detection method includes the following steps: S1, mixing the organic fertilizer sample with a buffer solution to obtain an extract; S2, adding a divalent calcium ion compound to the extract, mixing well, allowing it to stand, centrifuging, discarding the supernatant, and collecting the precipitate; S3, adding an alkaline releasing agent to the precipitate to dissolve it, centrifuging, collecting the supernatant, and obtaining a release solution; S4, reacting the release solution with a colorimetric reagent, measuring the visible light absorbance, and calculating the antibiotic content based on a standard curve. This method not only completely avoids the destruction of antibiotics by strong acids but also transforms humic acid from an interfering substance into an enrichment tool, thereby significantly improving the extraction rate. It is simple to operate and low in cost, thus providing a novel solution for the detection of macrolide antibiotic residues in organic fertilizers.

The present invention relates to an aminopyridone macrolide compound and the use thereof. Specifically disclosed is a compound represented by formula I or a pharmaceutically acceptable salt thereof. The compound of the present invention exhibits antibacterial, antimycoplasmal or antichlamydial activity, and can be used for preventing and / or treating related 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. Still further, the compound of the present application exhibits a superior antibacterial effect on Gram-positive bacteria. Even further, the compound of the present application exhibits a better inhibitory activity against mycoplasmas and a lower hepatotoxicity.

The application belongs to the field of macrolide polymerization, and relates to a diurea compound with an alicyclic structure, a preparation method, a catalyst system and a polymerization method. The structural formula of the diurea compound is as follows: in the formula, R is an alicyclic structure unit with C6-C18, R1 and R2 are each independently selected from at least one of a hydrogen atom, a C1-C20 alkyl group, a C3-C20 cycloalkyl group, a C6-C20 aromatic group and a substituted C6-C20 aromatic group. The application first proposes that a metal-free organic base / diurea catalyst system can be used to open ring polymerize macrolide polymerization and copolymerize macrolide and other cyclic monomers. The catalyst is easy to synthesize, low in cost, free of metal ions, low in polymerization temperature of the system, and mild in polymerization conditions, and can be used for polyhydroxyl prepolymers or block copolyesters of polyurethane, and has wide application and research value.

The present invention relates to the field of chemical synthesis. Disclosed are a method for synthesizing a key intermediate of a bryostatin compound and a method for synthesizing a bryostatin compound. The method for synthesizing a key intermediate comprises: dissolving a compound of formula (III) in a reaction solvent and then adding a Lewis acid for an intramolecular Prins cyclization reaction to obtain a compound of formula (IV). Iodination and carbonylation reactions are then carried out on an exocyclic double bond on a B ring to convert an olefin into an alkenoate compound; and after a key common intermediate is obtained, synthesis is enabled to separately obtain bryostatins 1, 7, and 9 and a bryostatin 9-N3 analogue, thereby achieving divergent synthesis of bryostatin analogues. The present invention realizes the specific selective construction of a cis-Z form of the B ring in bryostatin 1 by means of a ring-closing strategy of performing an esterification reaction on a C1 carboxyl group and a C25 hydroxyl group and simultaneously performing acetalization on a C15 aldehyde group and then constructing a macrocyclic lactone scaffold by means of gem-disilyl-mediated intramolecular stereoselective Prins cyclization.

Antibiotic compounds that are reaction products of an antibiotic molecule and a cross-linkable silane molecule are provided which are useful for incorporation into a liquid base coating material. The antibiotic molecule may be a fluoroquinolone, penicillin, cephalosporin, tetracycline, macrolide and / or aminoglycoside, while the cross-linkable silane molecule may be an epoxy-functionalized silane, an aldehyde-functionalized silane and / or a halogenated silane. Coating formulations including the antibioitic compounds and coated substrates which are coated with such coating formulations are also provided.

Provided are methods, compositions, and systems for detecting nucleic acids of macrolideresistant Mycoplasma genitalium. The illustrated method can involve real-time nucleic acid amplification, and further can involve processing real-time run curve data using a derivative-based analytical method to distinguish macrolide-resistant M. genitalium from macrolide-sensitive M. genitalium. Advantageously, the disclosed technique reduces the incidence of false-positive identification of macrolide resistance.

The invention belongs to the technical field of biological detection, genotype detection of a mutation site of Bordetella pertussis 23S rRNA A2047G is realized based on a PCR-melting curve method, and then macrolide antibiotic resistant Bordetella pertussis is detected, and the following technical scheme is adopted: the detection kit for the macrolide antibiotic resistant Bordetella pertussis has the advantages that the genotype of the mutation site of the Bordetella pertussis 23S rRNA A2047G mutation site is detected; the kit comprises a reaction solution, a detection solution, a sensitive positive control, a drug-resistant positive control and a blank control. The detection method comprises the following steps: S1, taking a bordetella pertussis DNA sample as a template, simultaneously using sensitive positive control, drug-resistant positive control and blank control, and using the macrolide antibiotic drug-resistant bordetella pertussis detection kit in the patent for detection; and S2, data processing: after the reaction is finished, performing result judgment through a melting curve of the sample.

The invention relates to a pyridone macrolide compound and application thereof. Specifically disclosed is a compound represented by formula I-1 or I-1 'or a pharmaceutically acceptable salt thereof. The compound disclosed by the invention has the activity of resisting bacteria, mycoplasma or chlamydia, and can be used for preventing and / or treating related diseases caused by bacteria, mycoplasma or chlamydia; furthermore, the antibacterial activity equivalent to or better than that of azithromycin or solificin can be achieved by using a lower dosage of the compound provided by the invention; furthermore, the compound provided by the invention has a better antibacterial effect on gram-positive bacteria; furthermore, the compound provided by the invention has better inhibitory activity and lower hepatotoxicity to mycoplasma.

The invention discloses a solid-phase extraction process method for detecting veterinary drug residues in an animal-derived sample, and belongs to the technical field of analysis of harmful residues in food. The method comprises the steps of sample pretreatment, solid-phase extraction column activation balance, sample loading, multi-stage washing and core collaborative elution. Especially, core collaborative elution adopts a collaborative elution method combining three-stage pH gradient elution and two-time competitive acetone pulse injection. The method comprises the following steps: firstly, eluting sulfonamides and quinolones under an acidic condition; then injecting acetone to competitively remove phospholipid; then, the tetracycline and macrolide drugs are eluted under the neutral condition; injecting acetone again for deep purification; and finally, eluting the chloramphenicol medicine under an alkaline condition. According to the method, the problem that the recovery rate and the purification degree are difficult to consider when multiple types of veterinary drug residues in the egg high-phospholipid complex matrix are synchronously detected is effectively solved, and the accuracy, the sensitivity and the reproducibility of subsequent LC-MS / MS analysis are remarkably improved.