Facile solid-phase ruthenium assisted azide-alkyne cycloaddition (RuAAC) utilizing the Cp∗RuCl(COD)-catalyst
作者:Ebbe Engholm、Nicolai Stuhr-Hansen、Ola Blixt
DOI:10.1016/j.tetlet.2017.04.095
日期:2017.6
The ruthenium assisted azide-alkyne cycloaddition (RuAAC) reaction is a well-established method for the generation of 1,5- and 1,4,5-substituted 1,2,3-triazoles, which we have extended to the solid-phase synthesis of 1,2,3-triazole-peptides. The 1,2,3-triazole moieties were formed upon the reaction of alkynes with a solid-phase bound secondary azide in the presence of the Cp∗RuCl(COD) catalyst at room
Use of a Compact Tripodal Tris(bipyridine) Ligand to Stabilize a Single-Metal-Centered Chirality: Stereoselective Coordination of Iron(II) and Ruthenium(II) on a Semirigid Hexapeptide Macrocycle
the Fe(II)–peptide complex has an apparent C3-symmetric conformations on the NMR time scale, while the peptide backbone is subject to dynamic conformational exchange between three asymmetric β/γ conformations and one C3-symmetric γ/γ/γ conformation. The semirigid cyclic hexapeptide preferentially arranged these conformations of the small octahedral Fe(II)–bipyridine complex, as well as the Ru(II) congener
设计并合成了含有三个2,2'-联吡啶部分作为侧链的Fe(II)配位六肽。具有三个[(2,2'-联吡啶)-5-基]甲环六肽- d -丙氨酸(d -Bpa5)残基,其中ð -Bpa5和甘氨酸交替排列用3重旋转对称,具有铁协调(II)形成具有金属中心手性的单个面部-Λ构型的1:1八面体Fe(II)-肽复合物。NMR光谱和分子动力学模拟表明,Fe(II)-肽配合物具有明显的C 3在NMR时标上具有对称的构象,而肽主链则在三个非对称的β/γ构象和一个C 3对称的γ/γ/γ构象之间进行动态构象交换。半刚性环状六肽优先排列小八面体Fe(II)-联吡啶配合物以及Ru(II)同源物的这些构象,以支撑以金属为中心的手性的单一构型。
[EN] BIORESPONSIVE POLYMER SYSTEM FOR DELIVERY OF MICROBICIDES<br/>[FR] SYSTEME POLYMERE BIOSENSIBLE POUR L'ADMINISTRATION DE MICROBICIDES
申请人:UNIV UTAH RES FOUND
公开号:WO2005097210A1
公开(公告)日:2005-10-20
The polymer systems of the present invention degrade in the presence of an ejaculate. They may further provide degradable sequences that degrade upon contact with an ejaculate and/or microbicides. The polymer systems of the present invention are of use in the oral, rectal or vaginal cavities of an individual for such purposes as the treatment or prevention of sexually transmitted disease, the prevention or promotion of fertility or for hormone replacement therapy.
TetRis: Applying click chemistry, a series of doxycycline–amino acidconjugates was synthesized. The C‐terminally linked phenylalanine derivative emerged as a highly selective effector for the reverse phenotype revTetR(B), and did not activate TetR. Interestingly, the test compound proved to be almost devoid of any antibacterial activity; which will be highly beneficial for future applications to control