31 results about "Antituberculars" patented technology

The invention discloses a separation and selection method of antibiotic antitubercular endophyte, which comprises the steps as follows, the preparation of antibiotic antitubercular plant tissue, the surface sterilization and the sterility test, the separation and the purification of the endophyte, the ferment of endogenetic fungi, the ferment of endogenetic bacterium, the process of the zymotic fluid, the process of the thalli, the selection of the effective antibiotic bacterial strains, the selection of the effective antitubercular bacterial strains and the preservation of the strains. The separation and selection method of antibiotic antitubercular endophyte ensures the realization of obtaining the effective antibiotic antitubercular matter from microorganisms, thanks to separation and selection method, a batch of effective bacterial strains are obtained.

The invention discloses a preparation method of a medicated slow-release degradable bone scaffold, which comprises the following steps: preparing a biological degradable polyester material (such as PLGA (poly(lactic-co-glycolic acid)) and a loaded antitubercular medicament (such as rifampicin or isoniazide) into PLGA microspheres containing the rifampicin or isoniazide, respectively mixing the PLGA microspheres containing the rifampicin or isoniazide with a biological medical adhesive, and molding with a mold, thus obtaining the medicated slow-release degradable bone scaffold. Having a certain porosity, the medicated slow-release degradable bone scaffold prepared by the preparation method is beneficial to the transportation and exchange of body water, inorganic salt and other nutrient substances and cell metabolism products, thereby being more beneficial to the normal growth and physiologic metabolism of bone cells, and providing an ideal place for the growth of bone tissues; and accompanied by the degradation of the PLGA, the medicament can be continuously released in the focal position and can be kept at a certain concentration, thereby inhibiting the growth of tubercle bacillus, and ultimately degrading the PLGA into carbon dioxide and water which are removed from the body through body metabolism.

The invention discloses an application of clinafloxacin amino derivatives and medicinal salts thereof in preparing antitubercular medicaments. In the structural general formula of the clinafloxacin amino derivatives, R is -(CH2)nNR<1>R<2>, -CH(CH2CH2XCH3)NH2, 2-pyrrolidyl or -OR3; n is 0 or 1; R1 and R2 are separately hydrogen, methyl, 2-hydroxyethyl, (R)-1-ethyl-2-hydroxyethyl, 2-aminoethyl, 3-(dimethylamino)propyl, hydroxyl, amino, methylamino, methoxyl or thiourea group; X is S or SO2; R3 is methyl or isobutyl; the compounds have certain inhibitory effect on standard sensitive strains, clinically isolated sensitive strains and clinically isolated drug-resistant strains of mycobacterium tuberculosis, the antitubercular activity of a part of compounds is stronger than that of ofloxacin and clinafloxacin and weaker than that of moxifloxacin, thus providing a new research direction for the antitubercular medicaments, and being beneficial to clinical treatment of tuberculosis.

The invention relates to a method for extracting live bacteria RNA in Mycobacterium tuberculosis and a detection kit thereof, and particularly provides a method for extracting live bacteria RNA in Mycobacterium tuberculosis and a detection kit which is used for the live bacteria RNA in the Mycobacterium tuberculosis and is obtained by applying the method and combining fluorescent quantitative PCR technology. The kit can accurately, sensitively and quickly identify dead bacteria and the live bacteria of the Mycobacterium tuberculosis, reduce the cost and shorten the detection time, and more importantly, the kit is the basis of studies such as the diagnosis of tuberculosis, medicinal susceptibility experiments, the monitoring of chemotherapy response, the screening of new antitubercular medicaments, the prevention of the tuberculosis and the like.

The invention relates to new application of a fluoroquinolone compound comprising a 7-(3-amino-4-oximido)-1-piperidyl substitutional group, in particular to application of 1-cyclopropyl-6-flurine-8-methoxyl-7-[(3-amino-4-methyl/ethyl oximido) piperidyl-1-group]-1,4-dihydro-4-oxo quinoline-3-carboxylic acid, or medicinal salt, hydrate and composition thereof in curing tuberculosis. Compared with the conventional clinic first-line antitubercular medicament (such as rifampicin) and a second-line antitubercular fluoroquinolones medicament (such as ciprofloxacin and the like), the fluoroquinolone compound has more excellent antitubercular mycobacteria activity.

An attenuated Salmonella typhi carrier vaccine carrying tubercular mycobacterium Ag85B is prepared through preparing prokaryotic recombinant expression plasmid pGEX-Ag85B, configuring eukaryotic recombinant expression plasmid pVAX1-Ag85B, and preparing said antitubercular vaccine. It can be orally taken.

An antimycobacterial combination and composition for treating tuberculosis are described. The compounds used are N-(3-[[4-(3-trifluoromethylphenyl)piperazinyl]methyl]-2-methyl-5-phenyl-pyrrolyl)-4-pyridylcarboxamide of formula (I) or a pharmaceutically acceptable non-toxic salt thereof

and an amount of one or more first line antitubercular drugs.

The invention discloses a screening method of a drug for resisting retention-state mycobacterium tuberculosis, which utilizes the change of the light absorption value of an enzyme-labeling instrumentdetection reaction system to judge the inhibition function to the activity of protein kinase G in a sample by adding the sample to be measured into an enzyme activity measuring system, thereby screening a drug for resisting the retention-state mycobacterium tuberculosis. The screening method selects the protein kinase G as a target point and is different from the pervious antitubercular drug whichmainly aims at bacteria with active growth and propagation. The invention aims at solving the difficult problem of long-term incubative infection of mycobacterium tuberculosis by aiming at bacteria which exists in host cells for a long time in a retention state.

The invention relates to an antitubercular injection and a preparation method thereof. The antitubercular injection comprises the following traditional Chinese medicinal materials: panax notoginseng,astragalus, drynaria, olibanum and myrrh as well as glucose containing auxiliary materials for injection, polysorbate and benzyl alcohol and is prepared by the following process steps: preparing a concentrated solution, centrifugally separating, heating, dissolving, finely filtering, and the like. The invention solves the technical problems of unstable product quality and great clinical side effect caused by low production efficiency, poor medicinal liquid clarity, overstandard endotoxin, and the like due to easy membrane block and penetration in the production process of the traditional Chinese medicinal injection. The antitubercular injection has the functions of supplementing qi, nourishing the blood, tonifying the kidney, strengthening the bones and promoting blood circulation by removing blood stasis and is suitable for various tuberculosis, such as pulmonary tuberculosis, osteoarticular tuberculosis, lymphatic tuberculosis, and the like as well as nodular leprosy and other diseases.

The invention belongs to the technical field of drug molecules and in particular relates to an application of mycobacterium tuberculosis gene Rv2498c in the antitubercular inhibitor screened target. The application is characterized in that the gene has the nucleotide sequence shown as SEQ. ID NO:1, and the encoded protein has the sequence of SEQ. ID NO:2. A virtual screening method is utilized, aiming at a natural primer activity center of Rv2498c, 20 small molecule compounds with a high affinity with the natural primer binding sites of the Rv2498c are screened from a small molecule compound database by operating a molecular docking program, two antibacterial compounds such as 66# triazine compound and a 70# quinoxaline compound are obtained, the 66# triazine compound has the name of 4-aniline-6-piperidine-1-yl-1-1,3,5-triazine-2(1H)-hydrazone; and the 70# quinoxaline compound has the name of N-allyl-N-[3-(allylimine)-1,4-dihydro-2-quinoxalineyl]amine). The antibacterial effects of the two compounds in mycobacterium tuberculosis are evaluated.

Invention provides antitubercular compounds selected from propargylated 1,2,3 triazoles of Formula I, wherein, X is sulfur (S) or a sulphone (A), n, m represent independently an integer O or 1, with the provision that when ‘n’ is 1, ‘m’ is 1; R1 is hydrogen; C1-C6 linear or branched alkyl group optionally substituted with aryl group; halogen; or aryl group optionally substituted with —OCH3, halogen, and nitro; R2 and R3 are selected from the group consisting of hydrogen, C1-C6 alkyl optionally substituted with heterocyclic ring of 5 to 6 ring atoms containing one to three hetero atoms selected from oxygen, sulfur, nitrogen, which may be substituted with alkyl, arylalkyl, linear or branched alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or allyl or propargyl groups consisting of 1 to 6 carbon atoms; Z is C1-C6 alkyl optionally substituted with heterocyclic ring of 1 to 6 ring atoms, containing one to three hetero atoms selected from oxygen, sulfur, nitrogen, which may be substituted with arylalkyl, linear or branched alkenyl, substituted alkenyl, alkynyl, substituted alkynyl allyl or propargyl groups consisting of 1 to 6 carbon atoms; with the provision that when ‘m’ is 1, and ‘n’ is zero; R1 is selected from the group consisting of hydrogen, halogen; C1-C6 linear or branched alkyl group optionally substituted with aryl group or aryl group optionally substituted with —OCH3, halogen, and nitro, R2 and R3 are selected from the group consisting of hydrogen, C1-C6 alkyl optionally substituted with heterocyclic ring of 5 to 6 ring atoms containing one to three hetero atoms selected from oxygen, sulfur, nitrogen, which may be substituted with alkyl, arylalkyl, linear or branched alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or allyl or propargyl groups consisting of 1 to 6 carbon atoms; Z is selected from the group consisting of halogen, C1-C6 linear or branched alkyl group optionally substituted with heterocyclic ring of 1 to 6 ring atoms, containing one to three hetero atoms selected from oxygen, sulfur, nitrogen, wherein the heterocyclic ring may further be substituted with halogen, alkyl, arylalkyl.

The invention discloses an isoniazid thiadiazine thione derivative, which solves the problem that the existing derivative has poor lipid solubility of active ingredient, and can not dissolve in water or can not highly disperse. The structure of the derivative can be presented by INH-THTT-R-THTT-INH, wherein ING represents the structure of isoniazid of antitubercular drug, THTT is a ring structure, and R is linear chain, non-linear chain or annular alkyl compound containing two primary amines (including alkyl structures of different substituent groups). The derivative can be prepared into highly-dispersed drug delivery system, including the dosage form of liposome, solid lipid nanospheres, niosomes, micro emulsion and the like. The derivative can not only improve the lipid solubility of isoniazid, but also hydrolyze and release isoniazid active compound in vivo, increases the penetrability of isoniazid cell, reduces the tolerance of isoniazid during therapy and improves the curative effect.

Belonging to the field of medical technology, the invention discloses a new use of tuberculosis chemotherapeutic drugs, i.e. application of tuberculosis chemotherapeutic drugs in treatment of psoriasis. According to the invention, through oral administration of isoniazide, rifampicin, and any one of the antitubercular drugs sodium aminosalicylate, pyrazinamide, ethambutol, moxifloxacin hydrochloride and levofloxacin hydrochloride by psoriasis patients, 95% or more of the psoriasis patients can have obviously alleviated symptoms in 6-10 weeks and can achieve recovery in 10-18 weeks, and after recovery, the consolidation therapy to the 28th week is a treatment cycle, and relapse hardly occurs, thus reaching the purpose of radical treatment of psoriasis. If psoriasis is caused by mycobacterium tuberculosis infection, the invention starts from the cause of psoriasis, completely changes the treatment concept of original psoriasis treatment drugs and achieves etiological treatment. Moreover,the tuberculosis chemotherapeutic drugs involved in the invention are cheap, thus alleviating the psoriasis patients' economic burden caused by long-term medication of psoriasis patients.