Abstract: The present disclosure related to a method for screening compounds having the ability to prevent, treat or reduce malodor development on body surfaces. In particular, the method screens for compounds having the ability of preventing sweat malodor development caused by malodor causing volatile acid compounds and/or malodor causing volatile sulphur compounds. The present disclosure is based on a sensitive analytical method to determine the presence of the precursors of malodor causing volatile acid compounds and/or malodor causing volatile sulphur compounds present in sweat, which are metabolised by bacteria, such as, for example, Cornebacteria or Staphylococci to malodor causing volatile acid compounds and malodor causing volatile sulphur compounds.

Abstract: The invention provides an improved method of synthesising derivatives of ?-D-glucopyranoside-containing polymers, such as chitin, chitosan, cellulose, amylose, pullulan, curdlan, inulin, guar gum or cyclodextrin. The method includes reacting a polymer of formula (III) with a cyclic imide to form a polymer of formula (I) thereby introducing a nitrogen functionality at the 6-position and providing access to 6-deoxy-6-amino-?-D-glucopyranoside-containing polymers.

Abstract: This invention is based on the discovery that homogeneous catalysts, [Rh(C2H4)2Cl]2 and/or [Rh(COD)2][BF4], can be used to produce spinetoram in higher yields at lower catalyst loadings as compared to previous methodologies. In addition, one or more phosphorus ligand donors can also be added to further increase yields/efficiency. The methods and/or systems provided herein enable cost-effective ways to produce spinetoram in large quantity with relatively simple procedures.

Abstract: The present invention relates to a procedure for the production of tiacumicin B comprising fermentation of a micro-organism capable of producing tiacumicin B, in particular of the species Dactylosporangium aurantiacum or Actinoplanes deccanensis, in a culture broth containing emulsifiers, such as ethoxylated castor oil, in combination with antifoaming products and vegetable oils.

Abstract: Novel pharmacological treatment of bacterial infectious diseases in humans by use of apramycin of formula (I) or apramycin derivatives having significantly low toxicity.

Abstract: The present invention provides methods of synthesizing moenomycin analogs of Formula (I). The present invention also provides compositions comprising a compound of Formula (I) and kits for synthesizing compounds of Formula (I).

Abstract: Provided herein are uses of genes for HOG, Ras and cAMP signal transduction pathways to treat fungal infection. To regulate the HOG pathway of Cryptococcus neoformans, roles of SSK1, TCO2, SSK2, PBS2, HOG1, ENA1 and NHA1 genes were investigated to find that a biosynthesis level of ergosterol is increased when these genes are inhibited. When the genes are inhibited, a large amount of ergosterol is distributed on a fungal cell membrane. Accordingly, since there are many working points of an ergosterol-binding antifungal agent, an efficiency of the ergosterol-binding antifungal agent can be considerably improved. To regulate the Ras and cAMP pathways of Cryptococcus neoformans, roles of RAS1, RAS2, CDC24, GPA1, CAC1, ACA1, PKA1, HSP12 and HSP122 genes were investigated to find that a sensitivity to a polyene- or azole-based drug is increased when these genes are inhibited.

Abstract: Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

Abstract: The present invention relates to antimicrobial agents. Some embodiments include compounds, compositions, methods of preparation, and methods of treatment using new aminoglycosides and aminoglycoside derivatives.

Abstract: The present disclosure pertains to antimicrobial compositions for intravenous administration to patients who have experienced a serious brain trauma, to reduce the risk of occurrence of post-trauma microbial infections. The antimicrobial compositions comprise an ?-galacytosylceramide compound and one or more excipients. The present disclosure also pertains to the use of ?-galacytosylceramide compounds for the manufacture of antimicrobial medicaments for intravenous administration to patients with serious brain traumas. The present disclosure also pertains to methods for the prophylactic use of the antimicrobial compositions to reduce the risks of occurrence of post-trauma microbial infections.

Abstract: The control of the microbial contamination during the sugar fermentation in the processes for obtaining alcohol is a very important action to increase the productivity of the alcoholic fermentation processes. The Saccharomyces cerevisiae yeast cells engage a very tough nutritional competition for the sugarcane juice with the bacteria (Lactobacillus sp and Acetobacter) and the wild yeasts. The proposed composition uses an antimicrobial agent of the guanidine family, such as for example, poly(hexamethyl biguanide), an antibiotic agent, and also a surfactant agent, to prevent the undesired microbial growth. The present invention further refers to the process for controlling the microbial contamination through the use of said agents.

Abstract: The present description discloses a novel biologically active ingredient of manuka honey. Specially, the present description discloses a compound represented by the following formula. In this formula, each of R1, R2 and R3 independently represents a hydrogen atom or optionally substituted C1-4 alkyl group, m represents an integer from 1 to 3, each of R4-m, R5-m and R6-m independently represents a hydrogen atom or optionally substituted C1-4 alkyl group, and each of R7, R8, R9 and R10 independently represents a hydrogen atom or optionally substituted C1-4 alkyl group.

Abstract: The present invention describes single drug entities, formed by connecting an antibiotic moiety via a linker with a non-steroidal anti-inflammatory drug (NSAID) moiety. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual antibiotic and NSAID drug.

Abstract: The present invention describes antibiotic conjugates. These single drug entities are formed connecting one antibiotic with another antibiotic. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs.

Abstract: The present invention relates to the total chemical synthesis of the monosaccharide 35# (R??H), the disaccharide 36# (R??H; R??H), the trisaccharide 37# (R??H; R??H; R???H) and the tetrasaccharide 1# (R??H; R??H; R???H) of the following general formula wherein R represents —Y—NH2Y represents a linker R? is H or R? is H or R?? is H or of the lipopolysaccharide from Neisseria meningitidis, as well as to the trisaccharide 37# and the tetrasaccharide 1#, to vaccines containing at least one of the saccharides 1#, 35#, 36#, and 37# and to the use of such vaccine for immunization against diseases caused by infection with bacteria containing the tetrasaccharide ?-GlcNAc-(1?2)-?-Hep-(1?3)-?-Hep-(1?5)-?-Kdo or the trisaccharide ?-Hep-(1?3)-?-Hep-(1?5)-?-Kdo or ?-GlcNAc-(1?2)-?-Hep-(1?3)-?-Hep, especially for immunization against meningitis, septicaemia, pneumonia and nasopharyngitis caused by Neisseria meningitidis.

Abstract: Compounds and methods for use in selectively inhibiting a lytic enzyme based on feedback inhibition are described. The conjugated compound serves as a substrate for a lytic enzyme. Cleavage of the conjugated compound by the lytic enzyme releases an inhibitor of the enzyme.

Abstract: A selective agent comprising a triclosan derivative for use in selective inhibition of non-target cells in a mixed population of target and non-target cells. Preferably the triclosan derivative is a glycoside derivative, more preferably a pyranoside derivative. Suitably a selective medium comprising said selective agent and methods of culturing cells using the selective agent are provided.

Abstract: A method is disclosed for the Agrobacterium-mediated germline transformation of soybean, comprising infecting split soybean seeds, with a portion of the embryonic axis, with Agrobacterium tumefaciens containing a transgene. The method can further comprise regenerating the explants produced from the transformation of the split soybean seeds comprising a portion of embryonic axis in vitro on selection medium.

Abstract: A compound having a structure expressed by the following Structural Formula (1), tautomers thereof, or salts of the compound or the tautomers.

Abstract: Antimicrobial compositions comprising one or more compound components generally recognized as safe for human consumption, and related methods of use, such compositions and methods as can be employed in a wide range of agricultural, industrial, building, pharmaceutical and/or personal care products and applications.

Abstract: Caprazene is provided which is the compound represented by the following formula (I) wherein Me stands for methyl group, and a 5?-N-alkoxycarbonyl or 5?-N-aralkyloxycarbonyl derivative thereof, and wherein said compound has the 1H-NMR and 13C-NMR data as set forth in Table 15.

Abstract: The present invention relates to compounds useful for the treatment or prevention of bacteria infections. The invention also provides pharmaceutically acceptable compositions containing the compounds and methods of using the compositions in the treatment of bacteria infections. The invention also provides processes for making the compounds of the invention. The compounds of the present invention are represented by the following structure of Formula A: wherein the variables are as described herein.

Abstract: Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R1, R2 or R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: The present invention provides novel bisphosphonate conjugates, pharmaceutical compositions comprising bisphosphonate conjugates and methods of using such analogs in the treatment of bone cancer, bone-related diseases, bone infection, bone inflammation, and diseases of the soft tissues surrounding bones.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: This invention relates to a compound of Formula 1A: or a pharmaceutically acceptable salt thereof; wherein R1 to R4, R7, R9 to R12 and Y are as defined herein. The invention further relates to pharmaceutical composition comprising said compound or a pharmaceutically acceptable salt thereof; and method of using same for reducing or reversing bacterial resistance to at least one aminoglycoside antibiotic.

Abstract: The present invention provides glycorandomized structures and combinatorial methods for rapidly generating a diverse library of glycorandomized structures, comprising incubating one or more aglycons and a pool of NDP-sugars in the presence of a glycosyltransferase. The glycosyltransferase may be one that is associated with or involved in production of natural secondary metabolites, or one which is putatively associated with or involved in production of natural secondary metabolites. The glycosyltransferase may show significant flexibility with respect to its NDP-sugar donors and/or its aglycons. NDP-sugar donors may be commercially available, or may be produced by utilizing mutant or wild type nucleotidyltransferases significant flexibility with respect to their substrates.

Abstract: Disclosed herein are polybasic bacterial efflux pump inhibitors containing boronic acid functionality and their methods of synthesis, methods of use, and pharmaceutical compositions. Some embodiments include methods of treating or preventing a bacterial infection by co-administering to a subject infected with bacteria or at risk of infection with bacteria the efflux pump inhibitor with another anti-bacterial agent.

Abstract: Aminoglycoside antibiotics of the formula are disclosed. The compounds are useful for treating bacterial infections, particularly infections resistant to known antibiotics.

Abstract: The present invention relates to pharmaceutical compositions for treatment of acne. In particular, the present invention relates to stable pharmaceutical compositions for treatment of acne along with other pharmaceutically acceptable excipients. These compositions exhibit excellent stability, greater permeability, and enhanced therapeutic efficacy. The invention also relates to processes for the preparation of such compositions.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I) or (II): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R1, R2, R3, R11 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Aminoglycoside antibiotics of the formula are disclosed. The compounds are useful for treating bacterial infections, particularly infections resistant to known antibiotics.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R11 and R12 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: The present invention relates to hydroxyalkyl starch (HAS) conjugates and to a method for preparing the hydroxyalkyl starch (HAS) conjugates, the hydroxyalkyl starch (HAS) conjugates comprising a hydroxyalkyl starch derivative and a cytotoxic agent, said conjugate having a structure according the following formula HAS?(-M)n wherein M is a residue of a cytotoxic agent, the cytotoxic agent comprising a carbonyl group, HAS? is a residue of the hydroxyalkyl starch derivative comprising at least one functional group X, n is greater than or equal to 1, and wherein the cytotoxic agent is linked via the carbonyl function present in the cytotoxic agent to the functional group X comprised in the hydroxyalkyl starch derivative, wherein the linkage via the carbonyl function is a cleavable linkage, which is capable of being cleaved in vivo so as to release the cytotoxic agent.

Abstract: The present invention provides novel glycopeptides antibiotic derivatives comprising a sugar residue (I) represented by the formula: (wherein n is an integer of 1 to 5: Sugs are each independently a monosaccharide, (Sug)n is a divalent sugar residue formed by binding of same or different 1 to 5 monosaccharides; RA1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, or optionally substituted cycloalkyl; and RE is OH or NHAc (Ac is acetyl)) is bound to an aromatic ring of the fourth amino acid residue in the glycopeptide skeleton. These derivatives have antibacterial activity against vancomycin-resistant bacteria.

Abstract: The present invention provides synthetic Moraxella catarrhalis lipooligosaccharide (LOS)-based oligosaccharides and conjugates containing various M. catarrhalis serotype-specific oligosaccharide antigens or various core M. catarrhalis oligosaccharide structures or motifs corresponding to one or more of the three major serotypes and/or members within a given serotype. The oligosaccharides may be synthesized by a chemical assembly methodology relying on a limited number of monosaccharide and disaccharide building blocks. The invention further provides M. catarrhalis LOS-based immunogenic and immuno-protective compositions and antibodies derived therefrom for diagnosing, treating, and preventing infections caused by M. catarrhalis.

Abstract: The invention relates to the use of ethylenediamine tetraacetic acid (EDTA) and its derivatives, i.e. its salts and complexes for prevention and treatment of bacterial intestinal diseases of pigs and for increasing the effects of antibiotics exerted in such diseases. The invention also relates to compositions for animal husbandry, i.e. to veterinary compositions and to feeds and drinks which can be consumed by pigs, comprising EDTA or its derivatives.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Z1, Z2, Z3, Z4, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R8 and R9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Abstract: A method for the treatment of myeloma and thymoma by administering a therapeutically effective dose of Mycobacterium indicus pranii with Cyclophosphamide. This disclosure generally relates to the field of cancer biology. More specifically, this disclosure relates to the immunotherapeutic treatment of myeloma and thymoma, using a combination of heat killed Mycobacterium indicus pranii and the widely administered chemotherapeutic drug, Cyclophosphamide. Mycobacterium indicus pranii has already shown its efficacy as an immunomodulator and has been safely administered to humans. The most common method of cancer management is the application of chemotherapeutic drugs which results in side-effects. At lower non-toxic doses Cyclophosphamide is not effective. The present disclosure discloses a method of improving efficacy of non-toxic doses of Cyclophosphamide by administrating it together with Mycobacterium indicus pranii. This disclosure is relevant for the treatment of other lymphomas as well.

Abstract: The present invention relates to novel compounds of formulae (I) and (II) and pharmaceutically acceptable salts thereof that are useful in the treatment and/or prevention of human and animal bacterial infections and associated diseases and conditions; compositions containing such compounds; derivation of such compounds by fermentation and isolation, partial synthesis and total synthesis; methods of inhibiting bacterial growth; methods of treating, preventing or controlling bacterial infection; biologically pure cultures of bacterial strains from which such compounds may be produced; and processes for preparing compositions containing such compounds.

Abstract: The present invention concerns methods and compositions for delivery of therapeutic agents to target cells, tissues or organisms. In preferred embodiments, the therapeutic agents are delivered in the form of therapeutic-loaded polymers that may comprise many copies of one or more therapeutic agents. In more preferred embodiments, the polymer may be conjugated to a peptide moiety that contains one or more haptens, such as HSG. The agent-polymer-peptide complex may be delivered to target cells by, for example, a pre-targeting technique utilizing bispecific or multispecific antibodies or fragments, having at least one binding arm that recognizes the hapten and at least a second binding arm that binds specifically to a disease or pathogen associated antigen, such as a tumor associated antigen. Methods for synthesizing and using such therapeutic-loaded polymers and their conjugates are provided.

Abstract: Improved antibiotic analogs, and synergistic combinations of antibiotics designed based on structural crystallographic analysis, are provided as well as pharmaceutical compositions that include these improved analogs and synergistic combinations, along with methods for their production and use. The synergistic combinations target neighboring sites in the ribosome demonstrating the importance of the corresponding ribosomal sites for development of clinically-relevant synergistic antibiotics.

Abstract: An inhibitor of heat shock protein 90 (HSP90) can include a coumermycin A1 analog having a structure that inhibits HSP90 greater than coumermycin A1. That is, the coumermycin A1 analog is not coumermycin A1. The coumermycin A1 analog can have an antiproliferative biological activity, which can be superior to coumermycin A1. The activity can include the coumermycin A1 analog inhibiting a C-terminus of HSP90.

Abstract: Seven novel antibiotic substances can be produced by cultivation of a microbial strain which has been isolated from a soil sample and which is designated as Microbispora sp. A 34030 (deposited under an access number FERM BP-10505 in terms of Budapest Treaty). These seven antibiotic substances are named as bispolide A1, bispolide A2, bispolide A3, bispolide B1, bispolide B2a, bispolide B2b and bispolide B3, respectively. These bispolides are each novel compounds which have a chemical structure as collectively represented by the general formula (III) shown below: These bispolides have each a high antibacterial activity against a variety of bacteria, particularly Gram-positive bacteria and their antibiotic-resistant strains, and hence these bispolides each are effective and useful for therapeutically treating bacterial infections of Gram-positive bacteria in humans and animals.

Abstract: Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLeX) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in preparing multimeric SLeX compositions. In particular, the disclosed SLeX compounds can be used to prepare selectin binding ligand conjugates by linking them to a reporter moiety, such as a contrast agent, a radiodiagnostic agent, or a cytotoxic or chemotherapeutic agent. The SLeX compounds and conjugates of the invention exhibit binding to selectin that is similar to native Sialyl LeX, and are, therefore, useful for diagnosing and treating selectin-mediated disorders and related conditions.

Abstract: A preparation of antibiotic hygromycin B with low cell toxicity and high purity, and methods of preparing such a preparation, are provided. More specifically, an isolated antibiotic hygromycin B with a purity of greater than 98% and impurities C, D and E individually less than 0.5% and impurity F less than 2%, as measured by HPLC, is described. Uses of this high purity antibiotic hygromycin B include, for example, for in vitro cell selection.

Abstract: The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side-effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.

Abstract: The present invention provides regio- and stereoselective oxidation of unactivated C—H bonds using an engineered mutant cytochrome P450 monooxygenase and an engineered substrate.