Document Detail

Novel design and synthesis of modified structure of carvedilol.
MedLine Citation:
PMID:  21834769     Owner:  NLM     Status:  MEDLINE    
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.
Mehrnoosh Hashemzadeh; Mohammad R Movahed; Wade A Russu; Ladan Soroush; Diné N Hill
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Publication Detail:
Type:  Journal Article    
Journal Detail:
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:
Created Date:  2011-09-12     Completed Date:  2012-01-13     Revised Date:  2013-05-28    
Medline Journal Info:
Nlm Unique ID:  101263805     Medline TA:  Recent Pat Cardiovasc Drug Discov     Country:  United Arab Emirates    
Other Details:
Languages:  eng     Pagination:  175-9     Citation Subset:  IM    
University of Arizona Sarver, Heart Center, 1501 North Campbell Avenue, Tucson, AZ 85724, USA.
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MeSH Terms
Adrenergic beta-Antagonists / administration & dosage,  chemistry*,  pharmacokinetics
Carbazoles / administration & dosage,  chemical synthesis,  chemistry*,  pharmacokinetics
Delayed-Action Preparations
Heart Failure / drug therapy,  physiopathology
Patents as Topic
Propanolamines / administration & dosage,  chemistry*,  pharmacokinetics
Reg. No./Substance:
0/8-fluoro-1,2,3,9-tetrahydro-4H-carbazol-4-one; 0/Adrenergic beta-Antagonists; 0/Carbazoles; 0/Delayed-Action Preparations; 0/Propanolamines; 0K47UL67F2/carvedilol

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