Document Detail


Synthesis of 2-(4-substituted benzyl-1,4-diazepan-1-yl)-N-(3,4-dihydro-3-oxo-2H-benzo[b][1,4]oxazin-7-yl)acetamides and their positive inotropic evaluation.
MedLine Citation:
PMID:  20591664     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Herein we describe the discovery of compound 3g, a potent positive inotropic agent compared with the standard drug, milrinone. Compound 3g was developed from a series of 2-(4-substitutedbenzyl-1,4-diazepan-1-yl)-N-(3,4-dihydro-3-oxo-2H-benzo[b][1,4]oxazin-7-yl) acetamides found in an evaluation of inotropic activity by measuring left atrium stroke volume on isolated rabbit heart preparations. Several compounds showed favorable activities, but 3g was the most potent, with 7.68+/-0.14% increased stroke volume (milrinone 2.38+/-0.05%) at 1 x 10(-5)M in our in vitro study. The chronotropic effects of compounds having significant inotropic effects were also evaluated.
Authors:
Kun Yang; Liang-Peng Sun; Ji-Yong Liu; Xun Cui; Hu-Ri Piao
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-06-15
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  20     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2010 Aug 
Date Detail:
Created Date:  2010-07-16     Completed Date:  2010-11-23     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  4464-7     Citation Subset:  IM    
Copyright Information:
Copyright 2010 Elsevier Ltd. All rights reserved.
Affiliation:
Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education, Yanbian University College of Pharmacy, Yanji 133000, PR China.
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MeSH Terms
Descriptor/Qualifier:
Acetamides / chemical synthesis,  chemistry*,  pharmacology
Animals
Azepines / chemistry*
Benzoxazines / chemistry*
Benzyl Compounds / chemistry*
Cardiotonic Agents / chemical synthesis*,  chemistry,  pharmacology
Heart Atria / physiopathology
Milrinone / pharmacology
Rabbits
Chemical
Reg. No./Substance:
0/1,4-diazepane; 0/Acetamides; 0/Azepines; 0/Benzoxazines; 0/Benzyl Compounds; 0/Cardiotonic Agents; 78415-72-2/Milrinone

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