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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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2Â¥2013-11-17 19:41:34
baiyuefei
°æÖ÷ (ÎÄѧ̩¶·)
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- LS-EPI: 1647
- Ó¦Öú: 4642 (¸±½ÌÊÚ)
- ¹ó±ö: 46.969
- ½ð±Ò: 658104
- É¢½ð: 11616
- ºì»¨: 995
- ɳ·¢: 81
- Ìû×Ó: 69424
- ÔÚÏß: 13328.4Сʱ
- ³æºÅ: 676696
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gruyclewee: ½ð±Ò+3, ¸ÐлӦÖú£¬½±ÀøÒ»Ï¡£ 2013-11-19 09:14:44
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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 |
3Â¥2013-11-17 19:41:47
baiyuefei
°æÖ÷ (ÎÄѧ̩¶·)
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- LS-EPI: 1647
- Ó¦Öú: 4642 (¸±½ÌÊÚ)
- ¹ó±ö: 46.969
- ½ð±Ò: 658104
- É¢½ð: 11616
- ºì»¨: 995
- ɳ·¢: 81
- Ìû×Ó: 69424
- ÔÚÏß: 13328.4Сʱ
- ³æºÅ: 676696
- ×¢²á: 2008-12-18
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4Â¥2013-11-17 19:42:16













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