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614 Newest Publications about the topic pharmacokinetic
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Synthesis, structure–property relationships and pharmacokinetic evaluation of ethyl 6-aminonicotinate sulfonylureas as antagonists of the P2Y12 receptor
10-06-2013 | Author(s): Peter Bach , Jonas Boström , Kay Brickmann , J.J.J. van Giezen , Robert D. Groneberg , Darren M. Ha ..., European Journal of Medicinal Chemistry, 2013
Publication date: July 2013 Source:European Journal of Medicinal Chemistry, Volume 65 Author(s): Peter Bach , Jonas Boström , Kay Brickmann , J.J.J. van Giezen , Robert D. Groneberg , Darren M. Harvey , Michael O'Sullivan , Fredrik Zetterberg The present paper describes the ...
Evaluation of thiazole containing biaryl analogs as diacylglycerol acyltransferase 1 (DGAT1) inhibitors
10-06-2013 | Author(s): Kishorkumar S. Kadam , Ravindra D. Jadhav , Shivaji Kandre , Tandra Guha , M. Mahesh Kumar Reddy , M ..., European Journal of Medicinal Chemistry, 2013
Publication date: July 2013 Source:European Journal of Medicinal Chemistry, Volume 65 Author(s): Kishorkumar S. Kadam , Ravindra D. Jadhav , Shivaji Kandre , Tandra Guha , M. Mahesh Kumar Reddy , Manoja K. Brahma , Nitin J. Deshmukh , Amol Dixit , Lalit Doshi , Shaila ...
Recent Trends and Future Prospects in Computational GPCR Drug Discovery: From Virtual Screening to Polypharmacology
05-06-2013 | Carrieri, Antonio; Perez-Nueno, Violeta I.; Lentini, Giovanni; Ritchie, David W., Current Topics in Medicinal Chemistry, 2013
Abstract: Extending virtual screening approaches to deal with multi-target drug design and polypharmacology is an increasingly important aspect in drug design. In light of this, the concept of accessible chemical space and its exploration should be reviewed. The great advantages of ...
p38 Mitogen-Activated Protein Kinase Inhibitors: A Review on Pharmacophore Mapping and QSAR Studies
05-06-2013 | Gangwal, Rahul P.; Bhadauriya, Anuseema; Damre, Mangesh V.; Dhoke, Gaurao V.; Sangamwar, Abhay T., Current Topics in Medicinal Chemistry, 2013
Abstract: p38 mitogen-activated protein (MAP) kinases are the serine/threonine protein kinases, which play a vital role in cellular responses to external stress signals. p38 MAP kinase inhibitors have shown anti-inflammatory effects in the preclinical disease models, primarily ...
Synthesis of Mixed (E,Z)-, (E)-, and (Z)-Norendoxifen with Dual Aromatase Inhibitory and Estrogen Receptor Modulatory Activities
03-06-2013 | Wei Lv; Jinzhong Liu; Deshun Lu; David A. Flockhart; Mark Cushman, Journal of Medicinal Chemistry, 2013
The first synthesis of the tamoxifen metabolite norendoxifen is reported. This included syntheses of (E)-norendoxifen, (Z)-norendoxifen, and (E,Z)-norendoxifen isomers. (Z)-Norendoxifen displayed affinity for aromatase (Ki 442 nM), estrogen receptor-α (EC50 17 nM), and estrogen receptor-β ...
A fast, sensitive, and high‐throughput method for the simultaneous quantitation of three ellagitannins from Euphorbiae Pekinensis Radix in rat plasma by ultra‐HPLC–MS/MS
30-05-2013 | Pengyi Hou, Yan Zeng, Bingjie Ma, Xiaofan Wang, Zhenzhen Liu, Lu Li, Kankan Qu, Kaishun Bi, Xiaohui Chen, Journal of Separation Science, 2013
A fast, sensitive and high throughput ultra‐HPLC–MS/MS method has been developed and validated for the simultaneous determination of three main active constituents of Euphorbiae Pekinensis Radix (EPR) in rat plasma. After addition of the internal standard, plasma samples were extracted by ...
1-Phenyl-4-benzoyl-1H-1,2,3-triazoles as Orally Bioavailable Transcriptional Function Suppressors of Estrogen-Related Receptor α
24-05-2013 | Shilin Xu; Xiaoxi Zhuang; Xiaofen Pan; Zhang Zhang; Lei Duan; Yingxue Liu; Lianwen Zhang; Xiaomei Ren; Ke Ding, Journal of Medicinal Chemistry, 2013
Estrogen-related receptor α is a potential candidate target for therapeutic treatment of breast cancer. We describe the discovery and structure–activity relationship study of a series of 1-phenyl-4-benzoyl-1H-1,2,3-triazoles as novel suppressors of ERRα transcriptional functions. The most ...
Discovery of Novel, Induced-Pocket Binding Oxazolidinones as Potent, Selective, and Orally Bioavailable Tankyrase Inhibitors
23-05-2013 | Howard Bregman; Nagasree Chakka; Angel Guzman-Perez; Hakan Gunaydin; Yan Gu; Xin Huang; Virginia Berry; Jingzhou Liu ..., Journal of Medicinal Chemistry, 2013
Tankyrase (TNKS) is a poly-ADP-ribosylating protein (PARP) whose activity suppresses cellular axin protein levels and elevates β-catenin concentrations, resulting in increased oncogene expression. The inhibition of tankyrase (TNKS1 and 2) may reduce the levels of β-catenin-mediated ...
Substrates and Controls for the Quantitative Detection of Active Botulinum Neurotoxin in Protease-Containing Samples
22-05-2013 | Karine Bagramyan; Bruce E. Kaplan; Luisa W. Cheng; Jasmin Strotmeier; Andreas Rummel; Markus Kalkum, Analytical Chemistry, 2013
Botulinum neurotoxins (BoNTs) are used in a wide variety of medical applications, but there is limited pharmacokinetic data on active BoNT. Monitoring BoNT activity in the circulation is challenging because BoNTs are highly toxic and are rapidly taken up by neurons and removed from the ...
An ultrasensitive chemiluminescent method for the tanshinol borneol ester determination and its pharmacokinetic analysis
17-05-2013 | Fei Nie, Min Bu, Lihong Wu, Jianbin Zheng, Luminescence, 2013
ABSTRACT Tanshinol borneol ester (DBZ), a chemical combination of danshensu and borneol, is an experimental drug that exhibits efficacious anti‐ischemic activity in animal models. In this work, an ultrasensitive chemiluminescence (CL) method for the determination of DBZ was established ...
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