245 words Tables: 6 Figures: 14 Abbreviations: ACh: acetylcholine; AMPA: -Amino-3-hydroxy-5-methyl-4isoxazolepropionic acid; DHPG: 3,4-Dihydroxyphenylglycine; DOPAC: 3,4Dihydroxyphenylacetic acid; GABA: gamma aminobutyric acid; 5-HT: 5-hydroxytryptamine or serotonin; 5-HIAA: 5-hydroxyindolacetic acid; LY341495: (2S)-2-amino-2-[(1S,2S)-2-carboxycycloprop-1-yl]-3-(xanth-9-yl) propanoic acid; mGl...

245 words Tables: 6 Figures: 14 Abbreviations: ACh: acetylcholine; AMPA: -Amino-3-hydroxy-5-methyl-4isoxazolepropionic acid; DHPG: 3,4-Dihydroxyphenylglycine; DOPAC: 3,4Dihydroxyphenylacetic acid; GABA: gamma aminobutyric acid; 5-HT: 5-hydroxytryptamine or serotonin; 5-HIAA: 5-hydroxyindolacetic acid; LY341495: (2S)-2-amino-2-[(1S,2S)-2-carboxycycloprop-1-yl]-3-(xanth-9-yl) propanoic acid; mGl...

(+)-Trans-(5R,6R)-5-bromo-6-ethoxy-5-ethyl-5,6-dihydro-2'-deoxyuridine [(5R,6R)-BEEDU], a po‌tential brain-targeted prodrug of 5-ethyl-2'-deoxyuridine (EDU), was synthesized by the regiospecific addition of BrOEt to the 5,6-olefinic bond of EDU. (5R,6R)-BEEDU is more lipophilic (log P = 0.04) than EDU (log P = -1.09). In vitro incubation of (5R,6R)-BEEDU with rat whole blood and brain ho‌mogena...

Siastatin B analogues, optically active 2-(trifluoroacetamide)- 3,4,5-trihydroxypiperidines having nitromethyl, aminomethyl and carboxyl branched groups at C-5, and (+)-(2R,3R,4R,5R)-5-(aminomethyl)-3,4,5-trihydroxy-2- (hydroxyacetamido)piperidine have been obtained total synthetically from D-ribono-1,4-lactone. Some analogues have inhibitory activity against some glycosidases, and (+)-(2R,3R,4...

(+)-trans-(5r,6r)-5-bromo-6-ethoxy-5-ethyl-5,6-dihydro-2'-deoxyuridine [(5r,6r)-beedu], a po tential brain-targeted prodrug of 5-ethyl-2'-deoxyuridine (edu), was synthesized by the regiospecific addition of broet to the 5,6-olefinic bond of edu. (5r,6r)-beedu is more lipophilic (log p = 0.04) than edu (log p = -1.09). in vitro incubation of (5r,6r)-beedu with rat whole blood and brain...

The study of the chemical constituents of the whole plant of Erigeron bonariensis (L.) has resulted in the isolation and characterization of a new and nine known compounds. The known compounds were identified as stigmasterol (1), freideline (2), 1,3-dihydroxy-3R,5R-dicaffeoyloxy cyclohexane carboxylic acid methyl ester (3), 1R,3R-dihydroxy4S,5R-dicaffeoyloxycyclohexane carboxylic acid methyl es...

A series of ratiometric probes based on heptamethine cyanine dyes for detecting hypochlorous acid have been developed. Here we present the synthesis, characterization and fluorescence properties of these probes. And it turns out that the probes are highly sensitive and selective toward hypochlorous acid. More importantly, the application in living cells for ratiometric imaging of hypochlorous a...

Methyladamantane and its derivatives are rare chemotypes for industrial even wide research use. The proposed scalable inexpensive approach to such compounds opens the door further extensive study of biologically active based on this uncommon core. Optimized synthesis key precursor, chiral (1S,3R,5R,7S)-3-methyl-5-phenyladamantane-1-carboxylic acid, showcases some significant innovations. main o...