The search for novel K+ channelopeners with a non-benzopyran skeleton, unlike cromakalim, led to the discovery of a new series of (Z)-2-(alpha-alkoxyimino)benzylpryridine derivatives. Synthesis was achieved by using a (Z)-dominant condensation reaction of benzoylpyridines with O-alkylhydroxylamines, followed by m-chloroperbenzoic acid (m-CPBA) oxidation. The compounds were tested for their vasorelaxant
Highly functionalized diaminocyclopentanes: A new route to potent and selective inhibitors of human O-GlcNAcase
作者:Patrick Weber、Zuzana Mészáros、Pavla Bojarová、Manuel Ebner、Roland Fischer、Vladimír Křen、Natalia Kulik、Philipp Müller、Miluše Vlachová、Kristýna Slámová、Arnold E. Stütz、Martin Thonhofer、Ana Torvisco、Tanja M. Wrodnigg、Andreas Wolfsgruber
DOI:10.1016/j.bioorg.2023.106819
日期:2023.11
A newclass of compounds inhibiting de-O-glycosylation of proteins has been identified. Highly substituted diaminocyclopentanes are impressively selective reversible non-transition state O-β-N-acetyl-d-glucosaminidase (O-GlcNAcase) inhibitors. The ease of preparative access and remarkable biological activities provide highly viable leads for the development of anti-tau-phosphorylation agents with a
已经鉴定出一类新的抑制蛋白质去-O-糖基化的化合物。高度取代的二氨基环戊烷是令人印象深刻的选择性可逆非过渡态O -β- N -乙酰基-d-氨基葡萄糖苷酶 ( O -GlcNAcase) 抑制剂。易于制备和显着的生物活性为抗 tau 磷酸化药物的开发提供了高度可行的线索,以期最终改善阿尔茨海默病。
Novel 6-oxo-6-naphthylhexanoic acid derivatives with anti-inflammatory and 5-lipoxygenase inhibitory activity
A series of novel 6-(6-alkoxy-2-naphthyl)oxoalkanoates and alkanamides were synthesized as inhibitors of inflammation and 5-lipoxygenase. They were evaluated in vivo for anti-inflammatory activity in the established adjuvent arthritis assay in rats and in vitro as inhibitors of 5-lipoxygenase in rat basophilic leukemia (RBL) cells. N-Hydroxy-N-methyl-6-(6-methoxy-2-naphthyl)-6-oxohexanamide, compound 28, which is representative of the more potent anti-inflammatory / 5-lipoxygenase inhibitors in the series was approximately twice as potent as the standard, ibuprofen in the adjuvent rat and exhibited an IC50 of 0.25 micromolar in the RBL assay.
Synthesis of a new series of N-hydroxy, N-alkylamides of aminoacids as ligands of NMDA glycine site
作者:E Ghidini
DOI:10.1016/s0223-5234(99)00222-6
日期:1999.9
DOLESCHALL, GABOR, TETRAHEDRON LETT., 28,(1987) N 26, 2993-2994