10.1021/jm8012882
The study focuses on the synthesis, biological, and physicochemical properties of novel isothiourea derivatives, specifically 3-allyl-1,1-dibenzyl-2-ethyl-isothiourea salts (1: hydrochloride, 2: hydrobromide, and 3: hydroiodide), which were developed as potential neuroprotectors and cognition enhancers. These compounds were evaluated for their ability to inhibit glutamate-stimulated calcium ion uptake in rat brain synaptosomes, interact with NMDA receptors, and their effects on AMPA receptor transmembrane currents induced by kainic acid and glutamate in Purkinje neurons. The study also included the growth of single crystals and X-ray diffraction experiments to determine the crystal structures of these salts, analysis of their solubility and partitioning properties in water and n-octanol, and assessment of their chemical stability in pH 7.4 phosphate buffer at 25 °C. The main purpose of these chemicals was to investigate their potential as therapeutic agents for neurological disorders by targeting ionotropic glutamate receptors, which play crucial roles in neuronal signaling, memory consolidation, and synaptic plasticity.
10.1007/BF00474003
The research focused on the synthesis and transformation of pyrido[2,3-d]pyrimidines, specifically oxo (hydroxy) derivatives, to explore their potential as biologically active compounds. The study involved the cyclization of 5-cyanoacetyl-6-aminouracils in acidic media, using reagents such as hydrobromic acid (HBr), hydrochloric acid (HCl), and sulfuric acid (H2SO4) to produce various pyrido[2,3-d]pyrimidines. The researchers also synthesized compounds with fixed structures, like 5,7-dimethoxy-, 7-methoxy-, and 5-ethoxypyridopyrimidines, and studied their spectral data. The study concluded that the synthesized pyrido[2,3-d]pyrimidines showed promising biological activity, with some exhibiting moderate inhibitory effects against certain types of cancer in animal experiments.
10.1021/ol901004e
The study presents a biomimetic synthesis of the dimeric metabolite acremine G, which was achieved through a highly regioselective and stereoselective Diels-Alder reaction between a TBS-protected hydroquinone diene and a structurally related alkenyl quinone. The synthesis involved the use of various chemicals, including toluhydroquinone as the starting material, iodine and silver trifluoroacetate for selective iodination, palladium(II) acetate and triphenylphosphine for the Heck coupling reaction, acetyl chloride and pyridine for dehydration to form the diene, and potassium fluoride, hydrobromic acid, and acetic acid for deprotection steps. These chemicals served the purpose of constructing the necessary precursors and facilitating the key Diels-Alder reaction, which led to the formation of acremine G after a series of transformations and deprotection steps. The study also proposed a mechanism for the oxidation of intermediates to acremine G, suggesting a radical pathway involving electron transfer to molecular oxygen.
10.1016/S0008-6215(00)81064-2
The research investigates the reduction products and bromodeoxy derivatives of dehydro-L-ascorbic acid phenylhydrazone (1), aiming to explore its synthetic potential and utility as a precursor to nitrogen heterocycles. Key chemicals used include sodium borohydride for reduction, hydrogen bromide for bromination, and reagents like phenylhydrazine, semicarbazide, and thiosemicarbazide for further derivatization. The study found that reduction of compound 1 with sodium borohydride yielded L-xylo-2-hexulosono-1,4-lactone phenylhydrazone (2), which was further acetylated to produce 5O-acetyl-3,6-anhydro-L-xylo-2-hexulosono-1,4-lactone phenylhydrazone (3). Bromination of 1 resulted in 5,6-dibromo-5,6-dideoxy-L-xylo-2,3-hexodiulosono-1,4-lactone phenylhydrazone (5), which could be reacted with various hydrazines to form bis(hydrazones) and semicarbazones. The conclusions highlight the versatility of dehydro-L-ascorbic acid phenylhydrazone as a synthetic intermediate for creating diverse nitrogen-containing compounds.
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