摘要:
Methods for preparing a glycopeptide are disclosed. The methods comprise the steps of selecting a protected glycopeptide of the formula A1-A2-A3-A4-A5-A6-A7, wherein the groups A1 to A7 comprise the heptapeptide structure of naturally occurring vancomycin; at least A4 is linked to a glycosidic group which has a hexose residue linked to A4; and the protected glycopeptide has no free amino or carboxyl groups and has a free primary hydroxyl group only at the 6-position of said hexose residue. The protected glycopeptide is contacted with a compound of the formula ArSO2G where Ar is an aryl group and G is a leaving group under conditions effective to allow reaction of said free primary hydroxyl group to form a glycopeptide sulfonate ester; and the glycopeptide sulfonate ester is contacted with a nucleophile under conditions effective to allow displacement of a sulfonate group to produce a substituted glycopeptide.
摘要:
A simple and efficient method of preparing a sample in the measurement according to matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS) capable of inhibiting any ion suppression by impurities, such as inorganic salts and surfactants, contained in the sample. An analyte and matrix molecules are co-crystallized in the presence of porous microparticles. Preferably, this co-crystallization is carried out by bringing the analyte, matrix molecules and porous microparticles into contact with each other on a target plate and thereafter drying the mixture. The porous microparticles consist of an ion exchanger having an average particle diameter of not more than 50 μm, preferably a strongly basic anion exchanger.
摘要:
A glycopeptide of the formula A1—A2—A3—A4—A5—A6—A7, in which each dash represents a covalent bond; wherein A1 comprises a modified or unmodified &agr;-amino acid residue, alkyl, aryl, aralkyl, alkanoyl, aroyl, aralkanoyl, heterocyclic, heterocyclic-carbonyl, heterocyclic-alkyl, heterocyclic-alkyl-carbonyl, alkylsulfonyl, arylsulfonyl, guanidinyl, carbamoyl, or xanthyl; wherein each of A2 to A7 comprises a modified or unmodified &agr;-amino acid residue, whereby (i) A1 is linked to an amino group on A2, (ii) each of A2, A4 and A6 bears an aromatic side chain, which aromatic side chains are cross-linked together by two or more covalent bonds, and (iii) A7 bears a terminal carboxyl, ester, amide, or N-substituted amide group; and wherein one or more of A1 to A7 is linked via a glycosidic bond to one or more glycosidic groups each having one or more sugar residues, at least one of the sugar residues bearing one or more substituents of the formula YXR, N+(R1)═CR2R3, N═PR1R2R3, N+R1R2R3 or P+R1R2R3 in which Y is a single bond, O, NR1 or S; X is O, NR1, S, SO2, C(O)O, C(O)S, C(S)O, C(S)S, C(NR1)O, C(O)NR1, or halo (in which case Y and R are absent). A chemical library comprising a plurality of the glycopeptides of the invention. A method for preparing a glycopeptide by glycosylation of an aglycone derived from a glycopeptide antibiotic. A method for preparing a glycopeptide by preparing a pseudoaglycone from a glycopeptide antibiotic and glycosylating the pseudoaglycone.
摘要翻译:式A1-A2-A3-A4-A5-A6-A7的糖肽,其中每个短划线代表共价键; 其中A1包含经修饰或未修饰的α-氨基酸残基,烷基,芳基,芳烷基,烷酰基,芳酰基,芳烷酰基,杂环,杂环羰基,杂环烷基,杂环 - 烷基 - 羰基,烷基磺酰基,芳基磺酰基,胍基,氨基甲酰基或 呫吨 其中A2至A7各自包含经修饰或未修饰的α-氨基酸残基,由此(i)A1与A2上的氨基连接,(ii)每个A2,A4和A6均带有芳香侧链,该芳族侧 链通过两个或更多个共价键交联在一起,和(iii)A7具有末端羧基,酯,酰胺或N-取代的酰胺基;并且其中A1至A7中的一个或多个通过糖苷键连接至 一个或多个糖苷基各自具有一个或多个糖残基,至少一个带有一个或多个式YXR,N +(R 1)= CR 2 R 3,N = PR 1 R 2 R 3,N + R 1 R 2 R 3或 其中Y是单键,O,NR1或S的P +,R1R2R3; X是O,NR1,S,SO2,C(O)O,C(O)S,C(S)O,C(S)S,C(NR1)O,C(O)NR1或卤素 一种含有本发明多糖的化学文库。一种通过糖衍生自糖肽抗生素的糖苷配基糖基化制备糖肽的方法。一种制备糖肽的方法,所述糖肽通过从 糖肽抗生素和糖基化假糖苷配基。
摘要:
A glycopeptide of the formula A1-A2-A3-A4-A5-A6-A7, in which each dash represents a covalent bond; wherein A1 comprises a modified or unmodified α-amino acid residue, alkyl, aryl, aralkyl, alkanoyl, aroyl, aralkanoyl, heterocyclic, heterocyclic-carbonyl, heterocyclic-alkyl, heterocyclic-alkyl-carbonyl, alkylsulfonyl, arylsulfonyl, guanidinyl, carbamoyl, or xanthyl; wherein each of A2 to A7 comprises a modified or unmodified α-amino acid residue, whereby (i) A1 is linked to an amino group on A2, (ii) each of A2, A4 and A6 bears an aromatic side chain, which aromatic side chains are cross-linked together by two or more covalent bonds, and (iii) A7 bears a terminal carboxyl, ester, amide, or N-substituted amide group; and wherein one or more of A1 to A7 is linked via a glycosidic bond to one or more glycosidic groups each having one or more sugar residues, at least one of the sugar residues bearing one or more substituents of the formula YXR, N+(R1)=CR2R3, N=PR1R2R3, N+R1R2R3 or P+R1R2R3 in which Y is a single bond, O, NR, or S; X is O, NR1, S, SO2, C(O)O, C(O)S, C(S)O, C(S)S, C(NR1)O, C(O)NR1, or halo (in which case Y and R are absent). A chemical library comprising a plurality of the glycopeptides of the invention.A method for preparing a glycopeptide by glycosylation of an aglycone derived from a glycopeptide antibiotic.A method for preparing a glycopeptide by preparing a pseudoaglycone from a glycopeptide antibiotic and glycosylating the pseudoaglycone.
摘要:
A simple and efficient method of preparing a sample in the measurement according to matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS) capable of inhibiting any ion suppression by impurities, such as inorganic salts and surfactants, contained in the sample. An analyte and matrix molecules are co-crystallized in the presence of porous microparticles. Preferably, this co-crystallization is carried out by bringing the analyte, matrix molecules and porous microparticles into contact with each other on a target plate and thereafter drying the mixture. The porous microparticles consist of an ion exchanger having an average particle diameter of not more than 50 μm, preferably a strongly basic anion exchanger.
摘要:
A glycopeptide of the formula A1-A2-A3-A4-A5-A6-A7, in which each dash represents a covalent bond; wherein A1 comprises a modified or unmodified α-amino acid residue, alkyl, aryl, aralkyl, alkanoyl, aroyl, aralkanoyl, heterocyclic, heterocyclic-carbonyl, heterocyclic-alkyl, heterocyclic-alkyl-carbonyl, alkylsulfonyl, arylsulfonyl, guanidinyl, carbamoyl, or xanthyl; wherein each of A2 to A7 comprises a modified or unmodified α-amino acid residue, whereby (i) A1 is linked to an amino group on A2, (ii) each of A2, A4 and A6 bears an aromatic side chain, which aromatic side chains are cross-linked together by two or more covalent bonds, and (iii) A7 bears a terminal carboxyl, ester, amide, or N-substituted amide group; and wherein one or more of A1 to A7 is linked via a glycosidic bond to one or more glycosidic groups each having one or more sugar residues, at least one of the sugar residues bearing one or more substituents of the formula YXR, N+(R1)═CR2R3, N═PR1R2R3, N+R1R2R3 or P+R1R2R3 in which Y is a single bond, O, NR1 or S; X is O, NR1, S, SO2, C(O)O, C(O)S, C(S)O, C(S)S, C(NR1)O, C(O)NR1, or halo (in which case Y and R are absent). A chemical library comprising a plurality of the glycopeptides of the invention. A method for preparing a glycopeptide by glycosylation of an aglycone derived from a glycopeptide antibiotic. A method for preparing a glycopeptide by preparing a pseudoaglycone from a glycopeptide antibiotic and glycosylating the pseudoaglycone.