Synthesis and biological evaluation of substituted indazolyl amide derivatives as S-adenosyl-L-homocysteine hydrolase inhibitors

A series of novel amide derivatives bearing an indazole moiety were synthesized and evaluated for their in vitro S-adenosyl-L-homocysteine hydrolase (SAHase) inhibitory activity. Among these compounds, 8b, 8m, 8r and 8w showed better or similar inhibitory effects compared to the positive control aristeromycin. These results provide a novel lead for the discovery of more potent non-adenosine analogs as SAHase inhibitors.     

Simultaneous determination of urinary metabolites of methoxypsoralens in human and Umbelliferae medicines by high-performance liquid chromatography

A high-performance liquid chromatography method has been developed for the determination of coumarins and furocoumarins (psoralens). Nine coumarins and furocoumarins are separated simultaneously on a Hypersil C(8) (25 cm x 4.6-mm i.d.) column with a gradient of methanol and acetonitrile aqueous solution as mobile phase at 1.0 mL/min with two-channel UV-vis absorbance detection. The limits of detection are 0.366, 0.219, 0.317, 0.440, 0.536, 0.300, 0.531, 0.531, 0.237, and 0.280 ng/mL for coumarin, 7-hydroxycoumarin, 7-methoxycoumarin, citropten (5,7-dimethoxycoumarin), 7-ethoxy-4-methylcoumarin, psoralen, xanthotoxin (8-methoxypsoralen), bergapten (5-methoxypsoralen), isopimpinellin (5,8-dimethoxypsoralen), and imperatorin (9-isopenteneoxypsoralen), respectively. Human urine is analyzed 1-6 days after ingestion of the oral Chinese medicines. This lead to the conclusion that the concentration of coumarins and furocoumarins is higher than that of the control urine. The coumarins and furocoumarins are detected at 312 and 249 nm, respectively.     

New synthesis of SKF 89976A

Substituted 4,4-diaryl-3-butenyl-1-amines are synthesized in nearly 34-47% overall yields starting from 3-hydroxypiperidine by the regioselective Baeyer-Villiger lactonization, Grignard addition and elimination sequence. This facile strategy was also used to synthesize racemic SKF 89976A.     

稀土掺杂SiO2与SiO2@Au纳米球

By using EDTA-lanthanide (Eu³⁺， Tb³⁺) coordination compound as precursor， multicolor luminescent SiO₂ nanoshperes were prepared. Also， without any pre-treatment to the surface of SiO₂ nanosphere， a facile strategy was developed for the synthesis of SiO₂@Au core-shell nanospheres.     

Efficient surface plasmon amplification from gain-assisted gold nanorods

We report on the efficient surface plasmon amplification by stimulated emission of radiation (spaser) from a gold nanorod coated with proper gain media. Numerical simulations show that the threshold of the nanorod-based spaser is nearly 1 order of magnitude lower than that of the core-shell nanosphere, which is verified by analysis with electrostatic theory. Furthermore, it is found that the nanorod-based nanosystem possesses unique optical properties such as wavelength tunability and polarization sensitivity.     

Synthesis and biological evaluation of novel SIPI-7623 derivatives as farnesoid X receptor (FXR) antagonists

Most of reported steroidal FXR antagonists are restricted due to low potency. We described the design and synthesis of novel nonsteroidal scaffold SIPI-7623 derivatives as FXR antagonists. The most potent compound A-11 (IC₅₀?=?7.8?±?1.1 μM) showed better activity compared to SIPI-7623 (IC₅₀?=?40.8?±?1.7 μM) and guggulsterone (IC₅₀?=?45.9?±?1.1 μM). Docking of A-11 in FXR’s ligand-binding domain was also studied.