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Bai-Jun Ye, Xue-Kun Liu, Sheng-Ming Jiang, Xun Cui*, and Hu-Ri Piao*. Synthesis of 2-(4-Substitutedbenzyl-[1,4]diazepan-1-yl)-N-(1-methyl-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamides as Inotropic Agents.
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gruyclewee: ½ð±Ò+3, ¸ÐлӦÖú£¬½±ÀøÒ»Ï¡£ 2013-11-19 09:14:44
Synthesis of 2-(4-Substitutedbenzyl-[1,4]Diazepan-1-yl)-N-(1-Methyl-4,5-Dihydro-[1,2,4]Triazolo[4,3-A]Quinolin-7-Yl)Acetamides as Inotropic Agents  
×÷Õß: Ye, BJ (Ye, Bai-Jun)[ 2 ] ; Liu, XK (Liu, Xue-Kun)[ 2 ] ; Jiang, SM (Jiang, Sheng-Ming)[ 2 ] ; Cui, X (Cui, Xun)[ 1 ] ; Piao, HR (Piao, Hu-Ri)[ 2 ]  
À´Ô´³ö°æÎï: CHEMICAL BIOLOGY & DRUG DESIGN  ¾í: 77   ÆÚ: 1   Ò³: 98-103   DOI: 10.1111/j.1747-0285.2010.01057.x   ³ö°æÄê: JAN 2011  
±»ÒýƵ´Î: 3 (À´×Ô Web of Science)  
ÒýÓõIJο¼ÎÄÏ×: 10      [ ²é¿´ Related Records ]     ÒýÖ¤¹ØÏµÍ¼ÒýÖ¤¹ØÏµÍ¼      
ÕªÒª: In an attempt to search for more potent positive inotropic agents, a series of N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(substitutedbenzyl-[1,4]diazepan-1-yl)acetamides were synthesized and evaluated for positive inotropic activity by measuring left atrium stroke volume in isolated rabbit heart preparations. Some of these derivatives exhibited favorable activity compared with the standard drug, milrinone, among which 2-(4-(4-methylbenzyl)-[1,4]-diazepan-1-yl)-N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3-a]quinolin-7-yl)acetamide (6m) was the most potent, increasing stroke volume by 8.38 +/- 0.16% (milrinone 2.45 +/- 0.06%) at 3 x 10-5 m. The chronotropic effects of those compounds having inotropic effects were also evaluated in this work.  
Èë²ØºÅ: WOS:000285065000012  
ÎÄÏ×ÀàÐÍ: Article  
ÓïÖÖ: English  
×÷Õ߹ؼü´Ê: [1; 2; 4]triazolo[4; 3-a]quinolines; 1; 4-diazepan; positive inotropic activity; stroke volume  
KeyWords Plus: HEART-FAILURE; MORTALITY; VESNARINONE; ATRIA  
ͨѶ×÷ÕßµØÖ·: Cui, X (ͨѶ×÷Õß) Yanbian Univ, Coll Preclin Med, Yanji 133000, Peoples R China.
  ÔöÇ¿×éÖ¯ÐÅÏ¢µÄÃû³Æ
    Yanbian University  

µØÖ·:  [ 1 ] Yanbian Univ, Coll Preclin Med, Yanji 133000, Peoples R China
  ÔöÇ¿×éÖ¯ÐÅÏ¢µÄÃû³Æ
    Yanbian University  
[ 2 ] Yanbian Univ, Coll Pharm, Minist Educ, Key Lab Nat Resources Changbai Mt & Funct Mol, Yanji 133000, Peoples R China
  ÔöÇ¿×éÖ¯ÐÅÏ¢µÄÃû³Æ
    Yanbian University  

µç×ÓÓʼþµØÖ·: cuixun@ybu.edu.cn; piaohuri@yahoo.com.cn  
»ù½ð×ÊÖúÖÂл:
»ù½ð×ÊÖú»ú¹¹ ÊÚȨºÅ
National Natural Science Foundation of China  30560177  

[ÏÔʾ»ù½ð×ÊÖúÐÅÏ¢][Òþ²Ø»ù½ð×ÊÖúÐÅÏ¢]   

This work was supported by the National Natural Science Foundation of China (No. 30560177).

³ö°æÉÌ: WILEY-BLACKWELL PUBLISHING, INC, COMMERCE PLACE, 350 MAIN ST, MALDEN 02148, MA USA  
Web of Science Àà±ð: Biochemistry & Molecular Biology; Chemistry, Medicinal  
Ñо¿·½Ïò: Biochemistry & Molecular Biology; Pharmacology & Pharmacy  
IDS ºÅ: 691FF
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WOS:000285065000012
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