Search Results - "Xu, Weiren"
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Discovery of Novel PI3Kδ Inhibitors Based on the p110δ Crystal Structure
Published in Molecules (Basel, Switzerland) (21-09-2022)“…PI3Kδ is a key mediator of B-cell receptor signaling and plays an important role in the pathogenesis of certain hematological malignancies, such as chronic…”
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Conjugated bile acids activate the sphingosine-1-phosphate receptor 2 in primary rodent hepatocytes
Published in Hepatology (Baltimore, Md.) (01-01-2012)“…Bile acids have been shown to be important regulatory molecules for cells in the liver and gastrointestinal tract. They can activate various cell signaling…”
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Study on the Effect of Three CYP2C9 Variants on Drug–Drug Interaction Related to Six Drugs In Vitro by LC–MS/MS Method
Published in Chromatographia (01-03-2022)“…The influence of genetic polymorphism of metabolic enzymes on drug–drug interactions (DDI) should be thoroughly investigated owing to its remarkable effect on…”
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Systematic Structure-Activity Relationship (SAR) Exploration of Diarylmethane Backbone and Discovery of A Highly Potent Novel Uric Acid Transporter 1 (URAT1) Inhibitor
Published in Molecules (Basel, Switzerland) (27-01-2018)“…In order to systematically explore and better understand the structure-activity relationship (SAR) of a diarylmethane backbone in the design of potent uric…”
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Synthesis and cytotoxic activity of novel 3-(1H-indol-3-yl)-1H-pyrazole-5-carbohydrazide derivatives
Published in European journal of medicinal chemistry (01-12-2011)“…A series of novel 3-(1H-indole-3-yl)-1H-pyrazole-5-carbohydrazide derivatives 4Ia-n, 4IIa-b and 6 were prepared by hydrazinolysis of ethyl…”
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Discovery of a Flexible Triazolylbutanoic Acid as a Highly Potent Uric Acid Transporter 1 (URAT1) Inhibitor
Published in Molecules (Basel, Switzerland) (16-11-2016)“…In order to systematically explore and understand the structure-activity relationship (SAR) of a lesinurad-based hit ( ) derived from the replacement of the S…”
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Novel Anthranilamide-Based FXa Inhibitors: Drug Design, Synthesis and Biological Evaluation
Published in Molecules (Basel, Switzerland) (14-04-2016)“…Factor Xa (FXa) plays a significant role in the blood coagulation cascade and it has become a promising target for anticoagulation drugs. Three oral direct FXa…”
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GLP-1 analogs containing disulfide bond exhibited prolonged half-life in vivo than GLP-1
Published in Peptides (New York, N.Y. : 1980) (01-06-2011)“…► GLP-1 analog (GLP17057) containing an inter-disulfide bond extended its half-life. ► The analog (GLP17057) remained the biological activity of GLP-1. ►…”
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The influence of genetic polymorphisms in drug metabolism enzymes and transporters on the pharmacokinetics of different fluvastatin formulations
Published in Asian journal of pharmceutical sciences (01-03-2020)“…The purpose of the present study was to investigate the impact of genetic polymorphism on fluvastatin pharmacokinetics. In addition, we compared the…”
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Inhibition of P-glycoprotein by HIV protease inhibitors increases intracellular accumulation of berberine in murine and human macrophages
Published in PloS one (23-01-2013)“…HIV protease inhibitor (PI)-induced inflammatory response in macrophages is a major risk factor for cardiovascular diseases. We have previously reported that…”
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Discovery of Flexible Naphthyltriazolylmethane-based Thioacetic Acids as Highly Active Uric Acid Transporter 1 (URAT1) Inhibitors for the Treatment of Hyperuricemia of Gout
Published in Medicinal chemistry (Shp-sariqah, United Arab Emirates) (01-05-2017)“…Gout is the most common inflammatory arthritis, which, if left untreated or inadequately treated, will lead to joint destruction, bone erosion and disability…”
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Design, synthesis and antibacterial activity of novel actinonin derivatives containing benzimidazole heterocycles
Published in European journal of medicinal chemistry (01-05-2009)“…A series of novel actinonin derivatives containing a benzimidazole heterocycle linked as amide isostere have been designed and synthesized. The structures of…”
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13
Design, Synthesis and Biological Activity of Tetrazole-bearing Uric Acid Transporter 1 Inhibitors
Published in Chemical research in Chinese universities (01-02-2017)“…Systematic structure-activity relationship(SAR) exploration of a moderately active tetrazole-bearmg lesinurad-based hit If led to the discovery of a potent…”
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Synthesis and preliminary antibacterial evaluation of 2-butyl succinate-based hydroxamate derivatives containing isoxazole rings
Published in Archives of pharmacal research (01-06-2010)“…Two series of novel 2-butyl succinate-based Hydroxamate derivatives containing isoxazole rings were synthesized, characterized and evaluated for antibacterial…”
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15
Effects of Astragaloside IV on heart failure in rats
Published in Chinese medicine (02-04-2009)“…Astragaloside IV (ASI) in Radix Astragali is believed to be the active component in treating heart failure. The present study aims to examine the effects of…”
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Discovery of 6-deoxydapagliflozin as a highly potent sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes
Published in Medicinal chemistry (Shp-sariqah, United Arab Emirates) (01-05-2014)“…Systematic mono-deoxylation of the four hydroxyl groups in the glucose moiety in dapagliflozin led to the discovery of 6-deoxydapagliflozin 1 as a more active…”
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Disulfide bond prolongs the half-life of therapeutic peptide-GLP-1
Published in Peptides (New York, N.Y. : 1980) (01-07-2011)“…► GLP-1 homodimeric analog (hdGLP1G10C) extended the biological half-life of GLP-1. ► hdGLP1G10C remained the biological activity of GLP-1. ► hdGLP1G10C showed…”
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A novel GLP-1 analog exhibits potent utility in the treatment of type 2 diabetes with an extended half-life and efficient glucose clearance in vivo
Published in Peptides (New York, N.Y. : 1980) (01-07-2011)“…► GLP-1 analog (GLP715a) containing an inter-disulfide bond and a Trp-cage extended its half-life. ► The analog (GLP715a) remained the biological activity of…”
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Synthesis and biological evaluation of 3-(1H-indol-3-yl)pyrazole-5-carboxylic acid derivatives
Published in Archives of pharmacal research (01-03-2011)“…A series of novel compounds bearing a 3-(1 H -indol-3-yl)pyrazole-5-carboxylic acid nucleus were synthesized. Analytical and spectral data confirmed the…”
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1-(5-Bromo-2-chlorophenyl)-2,2-dichloro-1-(4-ethoxyphenyl)cyclopropane
Published in Acta crystallographica. Section E, Structure reports online (01-03-2013)“…The asymmetric unit of the title compound, C17H14BrCl3O, contains two independent molecules with different dihedral angles between the benzene rings [79.2 (1)…”
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