Biomimetic protecting-group-free 2′, 3′-selective aminoacylation of nucleosides and nucleotides
作者:Sohyoung Her、Ronald Kluger
DOI:10.1039/c0ob00795a
日期:——
Aminoacyl phosphate monoesters can be prepared free of an amino-protecting group and used directly in lanthanum-promoted selective monoacylation of either the 2′ or 3′-hydroxyl of nucleosides and nucleotides. For example, phenylalanyl ethyl phosphate rapidly forms esters with either of the 2′ or 3′-hydroxyls of ribonucleosides and nucleotides in the presence of lanthanum ions in aqueous buffer. Oligomerization
Described here is the denovo design and synthesis of a series of 6H-dipyrido[1,2-e:2′,1′-i]purin-6-ones (DPs) as a new class of visible-light photoredox catalysts (PCs). The synthesized DP1–5 showed their λAbs(max) values in 433–477 nm, excited state redox potentials in 1.15–0.69 eV and −1.41 to −1.77 eV (vs. SCE), respectively. As a representative, DP4 enables the productive guanylation of various
本文描述了一系列 6 H-联吡啶并[1,2- e :2',1'- i ]purin-6-ones (DPs) 作为新型可见光光氧化还原催化剂的从头设计和合成(件)。合成的DP1-5的λ Abs(max)值分别在 433-477 nm,激发态氧化还原电位分别在 1.15-0.69 eV 和 -1.41 到 -1.77 eV(相对于SCE)。作为代表,DP4能够对各种胺进行有效的鸟苷化,包括 1°、2° 和 3°-烷基伯胺、仲胺、芳基和杂芳基胺、氨基腈、氨基酸和肽以及丙炔胺和 α-氨基酯,从而产生多样性在生物学上重要的胍和环状胍中。DP4在鸟苷酸化反应中的光催化功效超过了常用的 Ir 和 Ru 多吡啶基配合物,以及一些有机 PC。该方法的其他显着优点包括广泛的底物范围和官能团耐受性、克级合成和通用的后期衍生化,导致衍生物81对具有 IC 50的拉莫斯细胞表现出 60 倍更好的抗癌活性 比临床药物依鲁替尼
[EN] A SYNTHETIC CYCLIC DIPEPTIDE AND A PROCESS THEREOF<br/>[FR] DIPEPTIDE CYCLIQUE DE SYNTHÈSE ET PROCÉDÉ ASSOCIÉ
申请人:JNCASR BANGALORE
公开号:WO2011055247A1
公开(公告)日:2011-05-12
The disclosure relates to preparation and self-assembly of aromatic cyclic dipeptide into one and two dimensional nano, meso and micro structures. The said structures of cyclic dipeptide can be electrospinned into threads, fabrics, suture, bandage materials. They are also useful in cell culturing, tissue culturing, drug delivery system, as composite materials, as inhibitors of fibrillization and in Biomedical research such as neurological regeneration and organ replacement studies.
Novel spergualin-related compounds and process for producing the same
申请人:MICROBIAL CHEMISTRY RESEARCH FOUNDATION
公开号:EP0241797A2
公开(公告)日:1987-10-21
The present invention relates to novel Spergualin-related compounds represented by the general formula [I]
R2 is a residue obtained by removing, from an amino acid or peptide, the hydroxyl group of the carboxyl group and, when R, is a group other than -H, R2 is same as R, , or a pharmacologically acceptable salt thereof. Said compounds or salts thereof have an immune-modulating action.
The invention further relates to pharmaceutical formulations having an immuno-modulating activity which contain such Spergualin-related compounds and a process for the manufacture of these compounds and preparations.
本发明涉及由通式[I]表示的新型 Spergualin 相关化合物
R2 是通过从氨基酸或肽中去除羧基的羟基而得到的残基,当 R 是除-H 以外的基团时,R2 与 R 相同,或其药理上可接受的盐。上述化合物或其盐具有免疫调节作用。
本发明还涉及具有免疫调节活性的药物制剂,其中含有此类与 Spergualin 相关的化合物,以及制造这些化合物和制剂的工艺。
New spergualin-related compound and pharmaceutical composition
申请人:ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI
公开号:EP0309971A2
公开(公告)日:1989-04-05
The present invention relates to new spergualin-related compounds having an immunopotentiating effect and represented by the general formula [I]:
wherein X represents -(CH2)3-5- or
R represents -H or -CH2-OH and R1 and R2 each represents a residue formed by removing a hydroxyl group from the carboxyl group of an amino acid or peptide with the proviso that both of R1 and R2 cannot represent
at the same time,
and pharmacologically acceptable salts thereof.
本发明涉及具有免疫增强作用并由通式[I]表示的新的 spergualin 相关化合物:
其中 X 代表-(CH2)3-5-或
R代表-H或-CH2-OH,R1和R2各自代表通过从氨基酸或肽的羧基上除去羟基而形成的残基,但R1和R2不能同时代表
的残基、
及其药理上可接受的盐类。