Synthesis and anti-platelet aggregative activity of novel 2, 5-dihydrofuran derivatives

ZHONG Hanyu; ZHANG Yikai; ZHANG Jingyi; LI Ke

doi:10.3969/j.issn.1006-0111.2014.02.007

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Objective To study the synthesis and anti-platelet aggregative activity of 2-(4-methoxyphenyl)-4-vinyl-2,5-dihydrofuran-3-carboxylic acid derivatives. Methods 17 target compounds were designed, synthesized and determined via ¹H-NMR spectra and MS. The anti-platelet aggregative activities of the target compounds in vitro were assessed by Born method. Results The results of preliminary pharmacological test showed that all the target compounds had good anti-platelet aggregative activity in vitro and compounds 3, 6 and 10 were the best candidates, which had 22.2, 12.8 and 8.6 times than positive control, respectively. Conclusion 2-(4-methoxyphenyl)-4-vinyl-2,5-dihydrofuran-3-carboxylic acid derivatives had a pharmacological activity of anti-coagulation. The anti-platelet aggregative activities of compounds 3, 6 and 10 could be worth to further research.

Synthesis and anti-platelet aggregative activity of novel 2, 5-dihydrofuran derivatives

1. Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

2. Department of Pharmacy, General Hospital of Shenyang Military Region, Shenyang 110016, China

Received Date: 2012-04-24

Rev Recd Date: 2013-01-06

Key words:

Abstract: Objective To study the synthesis and anti-platelet aggregative activity of 2-(4-methoxyphenyl)-4-vinyl-2,5-dihydrofuran-3-carboxylic acid derivatives. Methods 17 target compounds were designed, synthesized and determined via ¹H-NMR spectra and MS. The anti-platelet aggregative activities of the target compounds in vitro were assessed by Born method. Results The results of preliminary pharmacological test showed that all the target compounds had good anti-platelet aggregative activity in vitro and compounds 3, 6 and 10 were the best candidates, which had 22.2, 12.8 and 8.6 times than positive control, respectively. Conclusion 2-(4-methoxyphenyl)-4-vinyl-2,5-dihydrofuran-3-carboxylic acid derivatives had a pharmacological activity of anti-coagulation. The anti-platelet aggregative activities of compounds 3, 6 and 10 could be worth to further research.

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[1]	杨曦明, 范聪, 李慧萍, 等. 白树花多糖硫酸酯的抗凝血活性研究[J]. 中国实验诊断学, 2010, 14 (7):1031.
[2]	Gardell SJ, Sanderson PE. Novel anticoagulants based on direct inhibition of thrombin and factor Xa[J]. Coron Artery Dis, 1998, 9 (2-3):75.
[3]	赵东明, 刘超美. 6-取代乙酰哌嗪苯基二氢哒嗪酮类化合物的合成及其抑制血小板聚集的作用[J]. 第二军医大学学报, 2003, 24 (5):510.
[4]	覃军, 王祥志, 刘毅敏. 6-(4-取代苯基)-5-甲基-4,5-二氢-3(2H)哒嗪酮类化合物的合成及其抑制血小板聚集的作用[J]. 化学研究与应用, 2006, 18 (9):1088.
[5]	周大铮, 易杨华, 毛士龙, 等. 香榧假种皮中的木脂素成分[J]. 药学学报, 2004, 39 (4):269.
[6]	Yang GM, Liu LM, Xu J. Effects of MCI-154 on vascular reactivity and its mechanisms after hemorrhagic shock in rats[J]. J Cardiov, 2006, 47 (6):751.
[7]	Kitada Y, Narimatsu A, Matsumura N, et al. Increase in Ca²⁺ sensitivity of the contractile system by MCI-154, a novel cardiotonic agent, in chemically skinned fibers from the guinea pig papillary muscles[J]. J Pharmacol Exp Ther, 1987, 243 (2):633.
[8]	Okafor C, Liao R, Perreault-Micale C, et al. Mg²⁺-ATPase and Ca²⁺ activated myosin ATPase activity in ventricular myofibrils from non-failing and diseased human hearts-effects of calcium sensitizing agents MCI-154, DPI 201-106, and caffeine[J]. Mol Cell Biochem, 2003, 245 (1-2):77.

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Synthesis and anti-platelet aggregative activity of novel 2, 5-dihydrofuran derivatives

doi: 10.3969/j.issn.1006-0111.2014.02.007

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