Synthesis of Biologically Active Piperidine Metabolites of Clopidogrel: Determination of Structure and Analyte Development
| Autor: | Animesh Goswami, Feng Qiu, Carl P. Decicco, Andrew T. Pudzianowski, Quentin Michaudel, Adrienne A. Tymiak, Patrick Y.S. Lam, Samuel J. Bonacorsi, Yingru Zhang, Benjamin P. Vokits, Bei Wang, Brad D. Maxwell, Bang-Chi Chen, Ronald L. Hanson, Jun Dai, Arvind Mathur, Dauh-Rurng Wu, Scott A. Shaw, W. Griffith Humphreys, Shun Su, Phil S. Baran, Janet Caceres Cortes, Balu Balasubramanian, Ruth R. Wexler, Zhiwei Guo, Rulin Zhao, Dawn Sun, Wenying Li, Li Peng, Kevin Cao |
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| Rok vydání: | 2015 |
| Předmět: |
Analyte
Ticlopidine Chemistry Metabolite Organic Chemistry Stereoisomerism Biological activity Prodrug Pharmacology Clopidogrel chemistry.chemical_compound P2Y12 Piperidines Biochemistry Microsomes Liver medicine Humans Prodrugs Platelet activation Platelet Aggregation Inhibitors Active metabolite Biological Phenomena medicine.drug |
| Zdroj: | The Journal of Organic Chemistry. 80:7019-7032 |
| ISSN: | 1520-6904 0022-3263 |
| Popis: | Clopidogrel is a prodrug anticoagulant with active metabolites that irreversibly inhibit the platelet surface GPCR P2Y12 and thus inhibit platelet activation. However, gaining an understanding of patient response has been limited due to imprecise understanding of metabolite activity and stereochemistry, and a lack of acceptable analytes for quantifying in vivo metabolite formation. Methods for the production of all bioactive metabolites of clopidogrel, their stereochemical assignment, and the development of stable analytes via three conceptually orthogonal routes are disclosed. |
| Databáze: | OpenAIRE |
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