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    
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.
Kun Yang; Liang-Peng Sun; Ji-Yong Liu; Xun Cui; Hu-Ri Piao
Related Documents :
23333444 - Concise synthesis of α-galactosyl ceramide from d-galactosyl iodide and d-lyxose.
24906414 - The volatome of aspergillus fumigatus.
23772914 - Synthesis of alkenyl boronates from allyl-substituted aromatics using an olefin cross-m...
24641574 - General allylic c-h alkylation with tertiary nucleophiles.
23333444 - Concise synthesis of α-galactosyl ceramide from d-galactosyl iodide and d-lyxose.
25162494 - Oxidative coupling of benzylamines to imines by molecular oxygen catalyzed by cobalt(...
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.
Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education, Yanbian University College of Pharmacy, Yanji 133000, PR China.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms
Acetamides / chemical synthesis,  chemistry*,  pharmacology
Azepines / chemistry*
Benzoxazines / chemistry*
Benzyl Compounds / chemistry*
Cardiotonic Agents / chemical synthesis*,  chemistry,  pharmacology
Heart Atria / physiopathology
Milrinone / pharmacology
Reg. No./Substance:
0/1,4-diazepane; 0/Acetamides; 0/Azepines; 0/Benzoxazines; 0/Benzyl Compounds; 0/Cardiotonic Agents; 78415-72-2/Milrinone

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

Previous Document:  Identification of novel alpha7 nAChR positive allosteric modulators with the use of pharmacophore in...
Next Document:  Synthesis and activity of polyacetylene substituted 2-hydroxy acids, esters, and amides against micr...