| Novel design and synthesis of modified structure of carvedilol. | |
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MedLine Citation:
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PMID: 21834769 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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β-adrenergic blocking agents have been in use for nearly 40 years. β-blockers have been more thoroughly studied in the past twenty years as they have become commonly prescribed to heart failure patients. The class of β-blockers has grown considerably and has many pharmaceutical applications in patients with heart failure. Carvedilol has been the most effective beta-blocker in the treatment of the systolic heart failure. Carvedilol is a non-selective β- and α-blocker enantiomer with antioxidant effects that are attributed to its carbazole moiety. Carvedilol is taken twice daily because it is extensively metabolized and therefore loses its effectiveness due to a short half-life. Recently a long acting carvedilol has become available, as Coreg CR. Coreg CR is available for once-a-day administration as controlled-release oral capsules containing 10, 20, 40, or 80 mg carvedilol phosphate. The subject of the current report is to design a new structural analog of carvedilol that incorporates a protecting group such as a fluorine atom at position 8 of the carbazole ring for the purpose of blocking a critical metabolic pathway thus increasing its half life. This will follow discussion regarding current carvedilol patents. We believe that carvedilol activity will remain unchanged. The synthesis of 8-Fluoro-1, 2, 3, 9- tetrahydro-4H-carbazol-4-one, a key synthetic intermediate of the designed carvedilol analog, was carried out and successfully characterized. |
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Authors:
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Mehrnoosh Hashemzadeh; Mohammad R Movahed; Wade A Russu; Ladan Soroush; Diné N Hill |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Recent patents on cardiovascular drug discovery Volume: 6 ISSN: 2212-3962 ISO Abbreviation: Recent Pat Cardiovasc Drug Discov Publication Date: 2011 Sep |
Date Detail:
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Created Date: 2011-09-12 Completed Date: 2012-01-13 Revised Date: 2012-01-16 |
Medline Journal Info:
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Nlm Unique ID: 101263805 Medline TA: Recent Pat Cardiovasc Drug Discov Country: United Arab Emirates |
Other Details:
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Languages: eng Pagination: 175-9 Citation Subset: IM |
Affiliation:
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University of Arizona Sarver, Heart Center, 1501 North Campbell Avenue, Tucson, AZ 85724, USA. mhashemzadeh@shc.arizona.edu |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Adrenergic beta-Antagonists
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administration & dosage,
chemistry*,
pharmacokinetics Animals Carbazoles / administration & dosage, chemical synthesis, chemistry*, pharmacokinetics Delayed-Action Preparations Half-Life Heart Failure / drug therapy, physiopathology Humans Patents as Topic Propanolamines / administration & dosage, chemistry*, pharmacokinetics |
| Chemical | |
Reg. No./Substance:
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0/8-fluoro-1,2,3,9-tetrahydro-4H-carbazol-4-one; 0/Adrenergic beta-Antagonists; 0/Carbazoles; 0/Delayed-Action Preparations; 0/Propanolamines; 72956-09-3/carvedilol |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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