Novel compound and Antibiotic Composition comprising the same
The present invention refers to novel antibiotic active compound and same antibiotic composition including a substrate compounds which inhibit microorganism lipid synthesis relates to the use of a compound and is. To treat diseases in which the infectious on a truly the intention to use antibiotic can last ten years have been increased significantly between in. 1954, of pounds of mask type color cathode ray only American antibiotic is produced. Today, was beyond the pounds pardon an on values. Central diseases according to control center (CDC), annual people and for circuit controlling isolation gates of 2 5 3 transition of antibiotics objects' traces to a consume. Dermatological or abuse a spread unchecked of antibiotic is antibiotic resistance in which raised, leading to severe sanitation. contribute to problem. Antibiotic resistance bacteria, which leads to the infection is to be used cease the infection by antibiotics using pin. accessing salvaged. Bacteria survive the more detrimental is the free surfaces and growing. For example, Staphylococci outer [...] aerodynamically-the (Staphylococcus aureus), , amongst to the antibiotic vancomycin reacting with the fluid on the hospital from infection is a main factor. However, former is greater than the Staphylococci outer in vancomycin strains have [...] was appears to be resistant. Furthermore, bacterial resistance to antibiotics is partially tuberculosis since the some infectious diesease death rate, such increased once again of wet liquid to flow down. Antibiotic a use in the treatment of bacterial infections used therapeutically of wet liquid to flow down. Classification according to electromotive of action, a plurality types of antibiotic is currently in use. The antibiotic types of known, number synthesis inhibitor wall such as cells, cell membrane number inhibitors, protein synthesis inhibitor effect on the syntheses RNA or DNA and number or affect included inhibitor binding to the same. Beta lactam antibiotics cells, such as wall synthesis inhibitor generally agent inhibit bacterial [...] some synthesis step. The penicillin, generally non-resistance (streptococcus) Streptococcal, Staphylococcal and gonococcus (staphylococcus) to efficient to (gonococcus). The gram-negative bacteria cancerous blood thread phosphorus and amoxicillin extensive exhibits spectrum over a. [...] surgical prophylaxis and gram-negative bacteria used for producing copper articles and which generally substitute penicillin for of wet liquid to flow down. Mono splitting a gourd in two, treatment individual-, free from allergy, and useful generally. Bacteria-related diseases and disorders treatment a plurality of suitable for use in, for example antibiotic The Physician ' s Desk Reference (PDR), Medical Economics Company (Montvale, NJ), (53rd Ed.), 1999 ; Mayo Medical Center Formulary, Unabridged Version, Mayo Clinic (Rochester, MN), January 1998 ; Merck Index: An Encyclopedia of Chemicals, Drugs and Biologicals, (11th Ed.), Merck & Co. , Inc. (Rahway, NJ), 1989 ; University of Wisconsin Antimicrobial Use Guide, http://www.medsch. Wisc. 5amcg/amcg/edu/clinsci. Html: Introduction on the Use of the Antibiotics Guideline, of Specific Antibiotics Classes, Thomas Jefferson University, http://jeffiine.tju. edu/CWIS/OAC/antibiotics guide/intro. Html; to been disclosure is publicly known. Xoo0880 in, the fabD Xoo of the most important drug target enzyme is one. A FabD gene expressing a Malonyl-CoA-acyl carrier protein transacylase (MCAT) enzyme (EC 2.3.1.39). This protein is a bacterial type II fatty acid in the synthesis to form an intermediate that is malonyl-ACP carrying-acyl a holographic to transmit site malonyl protein (Ruch, F. E. , And Vagelos, P. R. (1973). The present invention refers to said and of solving a problem with a conventional, need for said purpose of the invention the present so as by compounds that have a Hydrodisintegratable material the electrode 104 is provided under the. It is another object of the present invention including said compound by a rope. composition. To achieve the aim of said compounds of the present invention refers to formula 1 or its pharmaceutically acceptable salt provides. [Formula 1] Of the present invention in one embodiment, said compounds are malonyl-CoA: acyl carrier autodegradation [...] transport is the inhibition of the activity (MCAT) is preferably limited to but. can be realized. Also compounds of the present invention refers to said of the present invention formula 1 and a pharmaceutically acceptable carrier including medicament for treatment of or prevention of infection by pathogen compositions for the. In addition the present invention refers to said of the present invention formula 1 compounds and feed crane acceptable carrier including pathogen prevention of infection by provides a feed composition for preventing or treating. Also compounds of the present invention refers to said of the present invention formula 1 and a pharmaceutically acceptable carrier including infection compositions for the for preventing or treating. Of the present invention in one embodiment, said composition microorganisms lipid synthesis inhibitor preferably has an activity limited to but. can be realized. Pharmaceutical compositions in addition of the present invention number pharmaceutically acceptable excipients, carrier, diluent may include further such as. Liposomes include carrier available in the present invention, polysaccharide, polylactic acid, polyglycolic acid, polymerization body characteristic amino acids , and amino acid copolymer and slowly such as pharmacokinetics of macromolecules can be mentionned. For example, hydrochloride, hydrogel bromide, phosphate and sulfate such as salt of mineral acids; acetate, propionate, dichlorobenzoyl malonate and benzo, polycarbonate, to such as salt of an organic acid such pharmaceutically acceptable salts; water, brine, glycerol and a liquid, such as ethanol, and hydrophilizers, emulsion buffer pH or number and an adjuvant, such as material, use can be made of, either biological material,. Pharmaceutically acceptable literature with regard to carrier [Remingtion ' s Pharmaceutical Sciences, Mack Publishing Company, 1991] are depicted in. Furthermore, said pharmaceutical composition according to method of typically encountered in field within a patient's body for multiple type of the present invention show a release unit dosage suitable for administration by, preferably compound pharmaceuticals useful in administering the preparation form formulated in a dosage commonly used in the art for using method orally, or skin, intravenous, intramuscular, in artery, intramedullary, intraluminal water, in ventricular, waste, transdermal, avoid, , either intraperitoneally, intranasal, in an alimentary tract, topical, sublingual, vaginal or rectal path including parenteral administration can be degraded and is administered to the patient by path, limited to not. Bacteria therapeutically effective compound the capacitance approximately 1 kg weight receptor 1 0.1 to 50 0 mg or 0.1 to 200 mg, more generally receptor is 10.1 to about 100 mg per 1 kg weight. Pharmaceutically acceptable salt and prodrugs a passed reference range capacity effective metabolizable a parent compounds, based on the weight of. can be computed. Self [...] , the salts or prodrugs when active, effective the capacitance is created which is required to metabolizable, the salts or prodrugs said stated, to one skilled in the art or other publicly known means can be estimated by the. In the case of oral therapeutic administration, the active compound is in combination with one or more excipients taken tablet, buccally purification, key trough, capsule, [...] , suspension, syrup, for example, in such a form and it ladles, can be used. Purification, height system trough, bolus, one or more, or the like, that has number capsule can the following ingredients: coupled number, for example microcrystalline cellulose, [...] estradiol, acacia, maize starch gum or gelatin; number excipient, for example phosphoric acid this calcium , starch or lactose; disintegrating, for example maize starch, potato starches, alginate, such as (Primogel) gel [...] ; lubricant, for example magnesium stearate or [...] (Sterotes); composes a lubricant, for example colloidal silicon dioxide; sweetener, for example sucrose, fructose, lactose, saccharin or aspartame; flavor number, Mentha piperita for example, methyl salicylate, wintergreen oil or cherry direction; and peptide antibacterial number, for example [...] (FuzeonTM). When as capsule unit dosage form is, in addition to the type of material, vegetable oil or such as polyethylene glycol can a liquid carrier. A variety of other solid unit dosage form of zero or material is coated in order to alter the physical forms may be present. Pharmaceutical composition of the present invention suitable for rectal administration manufacturing formulations as, wrapping or can be commercially available. Such compositions for example, a suppository, solution for cleaning colon or rectum formulations and mobile terminal congestion may be in the form.. Pharmaceutical composition of the present invention for administering does in addition suitable for manufacturing formulations as, wrapping or can be commercially available. Such compositions for example, a suppository, vaginal inserts substance and depressed, e.g. tampon, cleaning formulations, solution for vagina wash balloon. may be in the form. Pharmaceutical compositions of the present invention adapted for administration to a eye formulations as manufacturing, wrapping or can be commercially available. In the case of topical administration, pure form compounds of the present invention, i.e. liquid can be applied. However, typically, acceptable carrier body picks data the skin compounds combined with skin as compositions or formulations can be administered to. Useful solid carrier a fine fraction which solid, e.g. talc, clay, microcrystalline cellulose, silica, includes alumina. Useful liquid vehicle, including water, alcohol, glycol, and two or more of these mixtures, optionally compounds of the present invention the non-toxic in effective level for using a surfactant can be dissolved or dispersed. The present invention according to a pesticide composition which comprises an further component, e.g. to yield agriculturally acceptable support, carrier or fillers may include further. In the present specification, a "support", an inverse plant parts in particular the active material a naturally occurring or synthetic, organic or non-organic exhibits inorganic material. Therefore, generally the supporting material and inert must of the substrate holding/acceptable. Photosensitive drum and charges the photosensitive drum can be solid or liquid. Examples of a suitable support, clay, natural or synthetic silicate, silica, resin, wax, solid fertilizer, water, alcohol, in particular butanol, organic solvent, solubilize mineral and and vegetable oils may be included a derivative thereof into a metal. Said of the support mixture can be used. In addition a pesticide composition which comprises an other can include additive components. In particular, a pesticide composition which comprises an further surfactant can. Surfactant number at least one ionic or non-ionic emulsifiers, dispersion number or a humectant or can be combination of. These include e.g. for example, polyacrylate salt, rig the Roh opinion phone it buys the salt , phenol the opinion phone it buys the saltthe opinion phone it buys the salt or naphthalene, ethylene oxide and fatty alcohol or fatty acid or fatty amine with polycondensate, substituted phenols (in particular alkylphenol or biting lung glow), [...] sulfoalkyl, taurine derivatives (in particular alkyl taurate), the phosphate ester with an alcohol or phenol along with ethyl polyoxyethylene, polyol fatty acid esters, and sulfate, sulfonate and said functional group-containing phosphate derivatives of the compounds in the. users can. Active ingredients and/or inert support is insoluble, an reagent vector apparatus and method for implementing time-when, , typically at least one surfactant is with an aldehyde in the presence of the presence of. Preferably, surfactant content of the composition can be 5 to 40 weight %. Additional components in addition, for example, protective colloids, adhesive, thickener, repayment (thixotropic agent), penetration number, stabilizer, can be includes sequestering agents. More generally, conventional active material formulated liquid additive solid or any of the art can be combined with. Generally, the present invention according to a pesticide composition which comprises an 0.05 to 99% (weight), preferably 10 to 70 weight % dose of active agent can. The present invention according to composition aerosol dispenser, capsule suspension, leucorrhea nothing concentrate, (dustable powder) committed, emulsifiable concentrate, an oil-in-water emulsion, water-in-oil emulsions, encapsulated granules, grained number, concentrate its fluid contents for seed treatment, gas (pressing the), gas generating product, granules, it comes nothing concentrate, macrocyclic granules, micro granules, oil dispersion powder, oil miscible flow concentrate, oil miscible liquid, paste, plant of small to (plant rodlet), drying powder for seed treatment, seed coated with pesticide, soluble concentrate, soluble powder, solution for seed treatment, suspension concentrate (flowable concentrate), small volume (ultra low volume; ulv) liquid, small volume (ulv) suspension, water-dispersible granular material or purification, treating slurries water-dispersible powder, soluble granule or purification, for seed treatment hydrophilizers and soluble powder and various forms, such as can be used. These compositions a suitable such as solution is sprayed or sprinkler device is processed using a device the in expense the applied directly to a plant or a seed that the as well as composition, before it is applied to crops to concentrate for commercial should be dilution includes compositions. Plant pathogenic bacteria of the present invention of a pesticide composition which comprises an the therapeutic or prophylactic treatment of repair as well as pour-on or prophylactic treatment of insect can be used. Therefore, according to one aspect of the present invention the additional, said effective of such a composition as defined in the non-phytotoxic amount seed treatment, applied leaves, stem applied, or seed, plant and/or plant fruit or plant growth or was growing is placed at the rear side of the substrate and/or inactivating soil (e.g.: to organic base materials (e.g.: sand, rock wool, glass wool, mortar (e.g.: perlite, vermiculite, zeolite, expandable clay)), inside pebble , [...] materials/admixtures, synthetic organic substrate (e.g.: polyurethane), organic-based (e.g.: peat, compost, the neck being waste (e.g.: coir, wood fiber/chip, in the bark of a tree)) and/or liquid based (e.g.: floating hydraulic system, Nutrient Film Technique, Aeroponics) applied (drench/drip) drip/irrigation to (irrigation) characterized by a carried out by using, of plant pathogenic bacteria to therapeutically or prophylactically exterminating insects as well as treating or prophylactically at controlling method is provided. Rotation "effective non-phytotoxic amount" or present in crop representation easily appeared for and/or disease the pest insects or while sufficient to, said phytotoxic significant no crop with or without also conditions the present invention according to. the amount of water composition. The or repellent the amount such pests and diseases, type of crop, the present invention according to and climatic conditions according to compounds to be compositions can be varied wide range of.. The amount said to be one can fix the are one skilled in the art, is provided with a bag-site, an effective in situ can be determining. Method processing the present invention according to the breeding material, e.g., as well as for treating rhizoma or tubers, seed, Young trees or implantation or implantation and plant Young trees useful in the treatment of plants as. In addition the method processing said can be as such, are useful in processing of the roots, wherein the. In addition the present invention according to the method processing associated plant body, stem or bag, leaves, flower and fruit and a plant such as ground-site to process a can be as such, are useful in. Protected by of the present invention method include cotton plants capable; flax ; (vine) plant creeper; fruit or vegetable crops, Young trees, chief crop, e.g. genus oryza (Graminae sp.) species (for example corn, lawn or wheat, rice, barley and ethylene isophthalate per-mill, such as grain), flower, horticultural crop exchanges; of these as well as homologues modified gene can be mentioned. Easily after adding salt compound or its in addition of the present invention a feed compositions, mammalian, avian, reptile, amphibian, fish animals, such as, a is carried out by using an acidulous feed which for. For example, two of the present invention the feed, CAT, PET food such as RAT, bovine, porcine such as of feedstuff for livestock, chicken, feed for poultry such as turkeys, american visit , defense such as is used as feed or similar for addtive, preferably PET food or of feedstuff for livestock is used as. Feed-material the feed of the present invention of the present invention to suitable compound or salt thereof can be made safely. Feed as cereal, bar steel current, vegetable type Pak type , animal feed-material, other feed-material, as to the aromatic hydrocarbon refined article. As cereal, to microresonator for example, mill, barley, oat, rye grass , brown rice, buckwheat, bath, transfer, pin, corn, soybean as to the aromatic hydrocarbon. As current bar, for example rice bran, degreasing rice bran, wheat bran, husk, mill, embryonic, barley bran, screening, pellets, corn bran, corn germ as to the aromatic hydrocarbon. As vegetable type Pak type , for example soybean foil, bean, flax foil, surface foil, peanut foil, safflower foil, plan foil, pak selling , the hormite foil, sunflower foil, the coleseed foil, pak width casing, as to the aromatic hydrocarbon mustard foil. Animal feed as, e.g. meal (north ocean mill, revenue mill, hole mill, Yan mill), brush fire fish, meat ingredient, [...] , [...] , decomposition parent, powdered bones , product processing for livestock, Federation mill, silkworm, is a skimmed milk powder, casein, whey as to the aromatic hydrocarbon drying. Other feed as plant foliage current (the egg it sells the green onion , detained cube, the egg it sells the green onion leaf powder and, acacia powder by similar), corn processing industrial product (cone gluten, mill, cone gluten feed, such as the above-mentioned tape car), starch workpiece, sugar, fermentation industrial product (yeast, beer foil, malt root, alcohol foil, soy sauce foil and has at least a polishing), agricultural residue (juice concentrate, such as a citrus processing foil, bean curd foil, coffee foil, cocoa foil and has at least a polishing), other (cassava, sleep two bean, acid mill, seaweed, methacrylic, Spirulina, chlorella, minerals) as to the aromatic hydrocarbon. refined article as protein (casein, such as albumin), amino acid, saccharide in the form of (starch, cellulose, [...] , such as glucose), mineral, vitamin as to the aromatic hydrocarbon. Through the present invention as will be seen, the present inventor are-ug/ml range bacteria on the growth inhibition of cells it has been discovered that the compound of 1. Figure 1 type II bacterial fatty acid synthesis pathway is indicative of the picture. Also electrophotographic SDS-PAGE fabD (Xoo0880) of purified has 2a and, 2b the 0.1 A non-limiting embodiment hereinafter to. rapidly and to reduce a memory further the present invention. Embodiment examples of the present invention relate to shear for the purpose of the present invention as disclosed and/or at least two different embodiment which is marked as a chemical range interpreted to limited. can be realized. Manufacturing e.g.: of the present invention for the preparation of Compounds used in the present invention are classified material Enamine Ltd (7 Deer Park Drive, Ste. M-3 Monmouth Jct, NJ 08852, USA) purchased from the specific gravity of 0.50 to 1.29 g, corresponding Company web site: is http://www.enamine.net/. In the embodiment 1: Xanthomona soryzae Cloning Xoo0880 FAD coding sequence of bacterial cells as a casting mold to thereby produce the use dielectric (Xoo KACC10331 strain) the frequency converter is filtered by an the polymerase chain reaction. Existing sequences primer [...] oligonucleotides reported gene been the device based on sequence (Lee, B. M. , Such as (2005) Overexpression and purification Xoo0880 pET11a-including His-TEV coding sequence of Crystallization and X-ray diffraction data collection Crystal screen HT °c, crystallization of XoMCAT, Index HT, Salt Rx HT (Hampton Research) and with the use of screening various such as tuned with an automated pipetting a been performed through Hydra II e-drop (Matrix), [high throughput (HT)] determined on 283K [...] been shown. Initially at very thin the acicular Wizard G-5 conditions determination (0.1 Crystal structure of XoMCAT also moieties of active sites of the resultant and was shown in 3. XoMCAT a total structure of a larger domain and a smaller domain consisting of domain two applicants fold in a stable manner; and a. A the active site the valley between the those domains. Domain greater DSSP program (Kabsch, W. And Sander, C. (1983). In the embodiment 2: target enzyme XoMCAT (VLS) process for virtual library screening the rice plant the white leaf in the bottle drying Xoo0880 (XoMCAT) based on the GlaxoSmithKline (GSK) for targeted likely since the one gene, high efficiency (HT) virtual library screening (VLS, also 4) XoMCAT through specific oligo-binding compounds drug against was searching. The ICM Molsoft modeling chute (suite) for screening drug a 1 million 8 transition a simulating computers by means of database compounds VLS performed. New solid during VLS Lipinski database compounds found through each flexible present in the substrate in a structure having a SIGE buffer layer of substrate binding pocket using ICM XoMCAT docking the n bit parallel data inputted to the electric power grid, complexes of was assigns a score of a mobile terminal, reflecting quality. Each substrate coupling result to check for playability of 3 times performed for all the parallel and simultaneously to. Top chart with the same each selecting compounds of 1991 a combination of complementary form (shape complementarity), hydrogen (flexibility) flexible and ligands combinational networks such as visualization coefficients (number of pixels having a value not) was the desired. Empirical analysis to characterize the final selection based on the step the 500 of compound is obtained. In the embodiment 3: Xoo, E A 3 ml of cultured during night Xoo NB of 100 ml was installed on both sides. Bacteria culture OD600 is good, until it reaches a 0.6 . 150 micro l of bacterial culture that was retrieved from a VLS [...] compound of 1 mm including 96 well ELISA plate moved. Compound 30 mm concentration of compound dissolved in DMSO which the first voice portion out of an. All bacterial growth assays DMSO concentration 5% hereinafter the n bit parallel data inputted maintained at, voice the control group only the first voice portion out of an same relevant concentrations of DMSO. While succussion occurs continuously the plate 28 in 600 nm absorbance culturing the cell line in the in 0, 3, 6, 9, and 12 have been measured by with a regular interval of time. Its compound with MIC50 value Xoo or more 50% to measure to inhibit growth those a vacuum. MIC50method (microtiter plates-based antibacterial analysis) A 3 ml of cultured during night Xoo NB of 100 ml was installed on both sides. Bacteria culture good until a cell density of standard 0.5 McFarland. Culture fluid having 10 times dilution and, a dilution of 150 micro l in the sterilized culture separating the 96-well clear flat bottom plate. High protein bacterial cell growth continuously a compound selected from the dilution concentration up to 9.5 M 600 M added to 96-well plate. Same relevant concentrations of DMSO the control group with voice culture bacteria having only a black and has in culturing the cell line in the plate. 28 °C, 20 hours OD600 measuring is performed for all the. Bacterial growth inhibitors of formula following percentage been calculated by. Inhibitors percent = 100 x (ODnc-ODtc) / (ODnc-ODpc) [ODnc: voice the control group of OD600, ODtc: of compounds and small molecules for their OD600, ODpc: positive the control group (the output of publicly known number) of OD600]. MIC50 values on the growth inhibition of cells bacteria of 50% a minimum decided to branch out into species concentration. Table 1 bacterial cell growth inhibition of compounds derived from analysis provided to MICs. foil. The present invention refers to novel antibiotic active compound and same antibiotic composition including a substrate compounds which inhibit microorganism lipid synthesis relates to the use of a compound and is. A compounds of formula 1 or its pharmaceutically acceptable salt. [Formula 1] According to Claim 1, said CoA-malonyl compounds: acyl carrier autodegradation [...] transport is the inhibition of the activity (MCAT) a compound or its pharmaceutically acceptable salt. Number 1 anti or according to Claim 2 compound and a pharmaceutically acceptable carrier or prevention of infection by pathogen including medicament for treatment of composition. According to Claim 3, said microorganisms composition active lipid synthesis inhibitor or prevention of infection by pathogens that medicament for treatment of composition. Number 1 anti or according to Claim 2 compound and including carrier acceptable feed crane pathogen prevention of infection by composition of feedstuff for or treatment. According to Claim 5, said composition microorganisms lipid synthesis inhibitor prevention of infection by pathogens that active composition of feedstuff for or treatment. Number 1 anti or according to Claim 2 compound and including agricultural chemical crane acceptable carrier composition for preventing or treating infection. Number 1 anti or according to Claim 2 activity including an antibacterial composition. ID Structure MIC50 (micro g/mL) T0506-8178 10
