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    Combinatorial library of moenomycin analogs and methods of producing same
    45.
    发明授权
    Combinatorial library of moenomycin analogs and methods of producing same 失效
    霉酚霉素类似物组合库及其生产方法

    公开(公告)号：US06114309A

    公开(公告)日：2000-09-05

    申请号：US975229

    申请日：1997-11-21

    申请人： Nigel Mark Allanson ,  Tin Yau Chan ,  Nicole T. Hatzenbuhler ,  Rakesh K. Jain ,  Ramesh Kakarla ,  Rui Liang ,  Dashan Liu ,  Domingos J. Silva ,  Michael J. Sofia

    发明人： Nigel Mark Allanson ,  Tin Yau Chan ,  Nicole T. Hatzenbuhler ,  Rakesh K. Jain ,  Ramesh Kakarla ,  Rui Liang ,  Dashan Liu ,  Domingos J. Silva ,  Michael J. Sofia

    IPC分类号： C12Q1/02 ,  A61K31/7016 ,  A61K31/702 ,  A61P31/04 ,  C07B61/00 ,  C07H1/02 ,  C07H5/08 ,  C07H11/04 ,  C07H15/04 ,  C07H15/203 ,  A61K31/70 ,  C07H13/00

    CPC分类号： C07H15/04 ,  C07H15/203 ,  C40B40/00

    摘要： A combinatorial chemical library of compounds structurally related to the moenomycin class of antibiotics has the formula ##STR1## wherein D is a donor mono- or disaccharide, A is an acceptor monosaccharide, and P-R is a lipophosphoglycerate mimetic group. Members of the library have a glycosidic linkage between the anomeric carbon of D and the C2 carbon of A, and the D-A moiety is in turn covalently linked through the anomeric carbon of A to the P-R group. Members of the library exhibit their greatest structural diversity in terms of substitutions occurring at the C3 position of the A residue, substitutions at the C2 position of the D residue, and different P-R groups used in assembling the compounds. Members of the library are preferably synthesized by solid phase techniques involving stepwise coupling of the respective units to a support, functionalizing the A and/or D saccharides either before or after immobilizing them on the support, and cleaving the assembled compounds from the support. Preferred functionalities attached to the sugar residues are amides, carbamates, ureas, sulfonamides, substituted amines, esters, carbonates, and sulfates. Exemplary P-R groups are derivatives of homoserine, glyceric acid, salicylates and mandelic acid. Members of the library can be screened for anti-microbial activity by contacting them with a culture of microbes and monitoring the growth rate of the microbes.

    摘要翻译： 结构上与新霉素类抗生素相关的化合物的组合化学文库具有下式：其中D是供体单糖或二糖，A是受体单糖，P-R是脂磷酸甘油酸酯模拟组。 文库成员在D的异头碳和A的C2碳之间具有糖苷键，D-A部分又通过A的端基异碳共价连接到P-R基团。 关于在A残基的C3位置发生的取代，在D残基的C2位置的取代以及用于组装化合物的不同的P-R基团，图书馆的成员表现出最大的结构多样性。 文库的成员优选通过固相技术合成，其包括将各单元逐步偶联到载体上，在将它们固定在载体上之前或之后将A和/或D糖功能化，并将载体化合物从载体上分离。 附着于糖残基的优选功能是酰胺，氨基甲酸酯，脲，磺酰胺，取代的胺，酯，碳酸酯和硫酸酯。 示例性的P-R基团是高丝氨酸，甘油酸，水杨酸盐和扁桃酸的衍生物。 通过与微生物培养物接触并监测微生物的生长速率，可以筛选图书馆成员的抗菌活性。