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Your search keyword '"Xiao, Zhi yan"' showing total 5 results
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5 results on '"Xiao, Zhi yan"'

1. [Design, synthesis and biological evaluation of oxadiazole derivatives as xanthine oxidase inhibitors].

Author

Yan DA, Zhang L, Tian JY, Ye F, and Xiao ZY

Subjects
Drug Design, Enzyme Inhibitors chemical synthesis, Febuxostat, Gout, Gout Suppressants chemical synthesis, Humans, Hyperuricemia, Enzyme Inhibitors pharmacology, Gout Suppressants pharmacology, Oxadiazoles pharmacology, Xanthine Oxidase antagonists & inhibitors
Abstract

Xanthine oxidase (XO) is an important target for the treatment of hyperuricemia and gout. Based on the two known non-purine xanthine oxidase inhibitors, febuxostat and topiroxostat, 14 oxadiazole derivatives have been designed and synthesized. These compounds have been evaluated against XO and five of them exhibited significant inhibitory activities at the concentrations below 10 μmol·L(-1).

Published
2016

2. [SAR of benzoyl sulfathiazole derivatives as PTP1B inhibitors].

Author

Yin WW, Chen Z, Tang YB, Ye F, Tian JY, and Xiao ZY

Subjects
Humans, Structure-Activity Relationship, Sulfathiazole, Sulfathiazoles chemistry, Protein Tyrosine Phosphatase, Non-Receptor Type 1 antagonists & inhibitors, Sulfathiazoles pharmacology
Abstract

Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. We have previously identified the benzoyl sulfathiazole derivative II as a non-competitive PTP1B inhibitor with in vivo insulin sensitizing effects. Preliminary SAR study on this compound series has been carried out herein, and thirteen new compounds have been designed and synthesized. Among them, compound 10 exhibited potent inhibition against human recombinant PTP1B with the IC50 value of 3.97 micromol x L(-1), and is comparable to that of compound II.

Published
2014

3. [Design, synthesis and evaluation of malonic acid-based PTP1B inhibitors].

Author

Du X, Zhang SE, Liu JZ, Nie FL, Ye F, Tian JY, and Xiao ZY

Subjects
Enzyme Inhibitors chemistry, Enzyme Inhibitors pharmacology, Humans, Inhibitory Concentration 50, Malonates chemistry, Malonates pharmacology, Molecular Structure, Protein Tyrosine Phosphatase, Non-Receptor Type 1 metabolism, Structure-Activity Relationship, Drug Design, Enzyme Inhibitors chemical synthesis, Malonates chemical synthesis, Protein Tyrosine Phosphatase, Non-Receptor Type 1 antagonists & inhibitors
Abstract

Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. Phosphotyrosine (pTyr) is the substrate for PTP1B dephosphorylation. Malonic acid moiety was used herein as a mimic of the phosphate group in pTyr, and novel malonic acid derivatives 1-7 were designed, synthesized and evaluated as PTP1B inhibitors. Results from enzymatic assays indicated that compounds 3 and 4 exhibited potent inhibition against human recombinant PTP1B with IC50 values of 7.66 and 1.88 micromol x L(-1), respectively.

Published
2012

4. [Design, synthesis and evaluation of novel 2H-1, 4-benzodiazepine-2-ones as inhibitors of HIV-1 transcription].

Author

Tang YB, Zhang CM, Fang C, Hu C, Huang L, Chen CH, and Xiao ZY

Subjects
Benzodiazepinones chemistry, Cell Line, Tumor, Humans, Transcription, Genetic drug effects, Benzodiazepinones chemical synthesis, Benzodiazepinones pharmacology, HIV Long Terminal Repeat genetics, HIV-1 genetics, tat Gene Products, Human Immunodeficiency Virus antagonists & inhibitors
Abstract

HIV-1 trans-activator of transcription (Tat) plays a critical role in HIV-1 transcription. Based on the beta-turn motif present in HIV-1 Tat, a series of novel benzodiazepine analogs were designed as beta-turn mimetics and prepared from p-chloro-nitrobenzene/2-phenylacetonitrile, p-toluidine/benzoyl chloride, or (Z)-7-nitro-5-phenyl-1H-benzo[e][1, 4]diazepin-2(3H)-one (nitrazepam) through different synthetic routes. Preliminary biological evaluation indicated that compound 30 exhibited inhibitory activity on HIV-1 tat-mediated LTR transcription with EC50 of 25.0 micromol x L(-1) and showed no obvious cytotoxic effects on TZM-BI cells under the concentration of 100 micromol x L(-1).

Published
2011

5. [Advances in novel anti-HIV-1 drugs and drug candidates: 2005-2008].

Author

Zheng PR, Xue H, Xiao ZY, and Liu G

Subjects
Acquired Immunodeficiency Syndrome drug therapy, Anti-HIV Agents chemistry, Anti-HIV Agents therapeutic use, HIV Fusion Inhibitors chemistry, HIV Fusion Inhibitors therapeutic use, HIV Infections drug therapy, HIV Integrase Inhibitors chemistry, HIV Integrase Inhibitors therapeutic use, HIV Protease Inhibitors chemistry, HIV Protease Inhibitors therapeutic use, Humans, Molecular Structure, Reverse Transcriptase Inhibitors chemistry, Reverse Transcriptase Inhibitors therapeutic use, Anti-HIV Agents pharmacology, HIV Fusion Inhibitors pharmacology, HIV Integrase Inhibitors pharmacology, HIV Protease Inhibitors pharmacology, HIV-1 drug effects, Reverse Transcriptase Inhibitors pharmacology
Abstract

HIV and AIDS remain as the crucial global health concern, therefore, research and development of novel anti-HIV-1 chemical therapeutics is still of paramount significance, which may be illuminated by cases of successful marketed drugs. Herein, we document the discovery and biological profile of new anti-HIV-1 drugs approved by FDA between 2005 and 2008 and some drug candidates are also discussed.

Published
2010

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