Biomedical subjects

Yong-zhou Hu

Publications and source records attributed to Yong-zhou Hu.

7 recordsLinked to original sources

PubMed2006

[Synthesis and AchE inhibitory activity of 2-phenoxy-indan-1-one derivatives].

AIM: To design and synthesize novel AchE inhibitors. METHODS: The condensation of 2-bromo-5, 6-dimethoxy-indan-1-one with various aminoalkyl phenols in the presence of K2CO3 and acetonitrile gave the corresponding title compounds, and the in vitro AchE and BchE inhibitory activities were evaluated by the modified Ellman method. RESULTS: Sixteen novel target compounds 8a - p were synthesized, their structures were confirmed by 1H NMR, MS, IR and elemental analysis. Preliminary pharmacological test demonstrated that most of these compounds displayed high AchE inhibitory activities, the IC50 of the most potent inhibitor 8h was 50.0 nmol x L(-1), similar to that of Huperzine A (IC50 = 53.0 nmol x L(-1)), while all the compounds were almost inactive against BchE. CONCLUSION: 2-Phenoxy-indan-1-one derivatives exhibit high activities of AchE inhibition and are worthy of further investigation.

Acetylcholinesterase↗

PubMed2005

[Synthesis and antitumor activity of arylsubstituted imidazolin-2-one derivatives].

AIM: To design and synthesize new arylsubstituted imidazolin-2-one analogues as antitumor compounds. METHODS: Arylsubstituted imidazolin-2-ones were prepared by condensation the appropriate omega-amino-acetophenone hydrochloride with arylisocyanate in toluene. The target compounds prepared in this study were tested for cytotoxicity against PC-3, A549, HO-8910, Hela, HL60, K562 and HL60R cancer cell lines, and mechanism of one of the products 4y was further evaluated with its mechanium. RESULTS: Thirty-six new compounds were synthesized and confirmed by 1H NMR, MS and elemental analysis. One of the synthesized products, compound 4y, displayed an encouraging selective activity against HL60 cells, and it was partlydue to the cell cycle arrest and cell apoptosis. CONCLUSION: Compound 4y is worthy to be intensively studied.

Amides↗

PubMed2005

[Synthesis and vasorelaxation action of flavonoids].

AIM: To search for flavonoids which possess stronger vasorelaxation action. METHODS: Four quercetin glycosides (1a - d) were synthesized from quercetin in three steps i. e. selective protection of quercetin, condensation with corresponding acetyiglycosyl bromide, and then removal of the protecting group; Six flavone compounds (2a - f) were prepared from phloroglucinol according to the conventional methods; The structures of synthetic compounds were confirmed by IR, 1H NMR, 13C NMR and MS. Vasorelaxation action of ten synthetic quercetin derivatives (or analogues) and four natural flavonoids compounds were examined on the isolated rat thoracic aorta rings; Comparative octanol-water partition coefficients (logP) were measured using a reversed-phase HPLC method. RESULTS: Most of the tested flavonoids showed concentration dependent relaxation effects against PE-induced contractions of rat aortic rings. These compounds had stronger action with the augment of logP values. CONCLUSION: Compound 3-bromo-5 ,7-dihydroxyflavone (2d) was identified to have the most potent vasodilating action. These compounds exert vasodilating effects that are related to the logP values. A structure-activity relationship of flavonoids was suggested.

Animals↗

PubMed2004

[An improved novel method of venlafaxine synthesis].

OBJECTIVE: To synthesize venlafaxine with an improved novel method. METHODS: p-methoxypheny lethyl-acid was reacted with SOCl(2) to produce acyl chloride which was reacted with N,N-dimethylamine solution to get amide; then through Ivanov reaction and reduction by KBH(4)/BF(3).Et(2)O to yield venlafaxine. RESULT: Venlafaxine was successfully synthesized by using this method with an yield rate of 50.3%. CONCLUSION: The improved method is suitable for industrial production of venlafaxine.

Antidepressive Agents, Second-Generation↗

PubMed2004

[Study on ultrasonic extraction techniques of flavonoids in Chrysanthemum morifolium].

OBJECTIVE: To optimize the ultrasonic extraction condition for flavonoids from Chrysanthemum morifolium. METHOD: The extraction rate of flavonoids optimized condition (ethanol concentration, ultrasonic time, solvent quantity and extraction times) was determined by orthogonal design. UV-Spectrophotometry was used for the determination. RESULT: The order of factors to affect the flavonoid extraction was ethanol concentration > extraction times > solvent quantity > ultrasonic time. CONCLUSION: The optimum ultrasonic extractions were: A2 B2 C3 D3. Compared with traditional extraction, ultraction method can save time, be easy to operate, improve extraction rates and need no heating.

Chrysanthemum↗

PubMed2003

[Improved method of epalrestat synthesis].

OBJECTIVE: To synthesize epalrestat and to improve the method of synthesis. METHODS: Glycine reacted with carbondisulfide,then with ClCH(2)COONa to give 3-carboxymethylrhodanine. PhCHO reacted with CH(3)CH(2)CHO in NaOH/EtOH solution to produce 2-methylcinnamaldehyde.3-carboxymethylrhodanine and 2-methylcinnamaldehyde were treated with NH(3).H(2)O to obtain epalrestat. RESULT: The described method was effective in synthesis of Epalrestat and the yield was higher than that of in references. CONCLUSION: The results suggest that this method is suitable for industrial production.

Aldehyde Reductase↗

PubMed2003

[Improved method of fluvoxamine synthesis].

OBJECTIVE: To modify the synthetic method of fluvoxamine. METHODS: Fluvoxamine was synthesized from 4-trifluoromethylbenzonitrile by the steps of Grignard reaction, hydrolysis and oximation. RESULT: The chemical structure of the synthesized product was confirmed by (1)HNMR, and the total yield reached to 36.16%. CONCLUSION: The results indicate that the synthetic route is practical.

Fluvoxamine↗