Synthesis, QSAR and Calcium Channel Antagonist Activity of New 1,4-Dihydropyridine Derivatives Containing 1-Methyl-4,5-dichloroimidazolyl Substituents.

Hosseini M; Miri R; Amini M; Mirkhani H; Hemmateenejad B; Ghodsi S; Alipour E; Shafiee A

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Synthesis, QSAR and Calcium Channel Antagonist Activity of New 1,4-Dihydropyridine Derivatives Containing 1-Methyl-4,5-dichloroimidazolyl Substituents.

机译：含1-甲基-4,5-二氯咪唑基取代基的新型1,4-二氢吡啶衍生物的合成，QSAR和钙通道拮抗活性。

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A group of dialkyl and diarylester analogues of nifedipine, in which the ortho-nitrophenyl group at position 4 was replaced by a 1-methyl-4,5-dichloroimidazolyl substituent, were synthesized and evaluated as calcium-channel antagonists using the high K(+ )concentration of guinea-pig ileum longitudinal smooth muscle. The structure of all compounds was confirmed by IR,( 1)H-NMR, and mass spectra. The calcium-channel antagonist activity of compounds 10a-f demonstrated that compound 10b was the most active and 10f the least active one. With unsymmetrical diesters 12a-k, the most active compound was the ethyl, phenethyl derivative. Structural parameters on the calcium-channel antagonist activity were evaluated by QSAR analysis and a linear correlation was found between the -log IC(50) values of these compounds and their constitutional and topological properties.

机译：合成了一组硝苯地平的二烷基和二芳基酯类似物，其中第4位的邻硝基苯基被1-甲基-4,5-二氯咪唑基取代基取代，并使用高K（+ ）豚鼠回肠纵向平滑肌的浓度。通过IR，（1）H-NMR和质谱确认所有化合物的结构。化合物10a-f的钙通道拮抗活性表明，化合物10b活性最高，而10f活性最低。对于不对称的二酯12a-k，活性最高的化合物是乙基苯乙基衍生物。通过QSAR分析评估了钙通道拮抗剂活性的结构参数，发现这些化合物的-log IC（50）值与其组成和拓扑特性之间存在线性关系。

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来源
《Archiv der Pharmazie》 |2007年第10期|共8页
作者
Hosseini M; Miri R; Amini M; Mirkhani H; Hemmateenejad B; Ghodsi S; Alipour E; Shafiee A;
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正文语种 eng
中图分类药学;
关键词
Quantitative Structure-Activity Relationship; Calcium; Synthesis; Endurance of activity; 钙;

机译：定量构效关系;钙;合成;活度;钙;

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1. Synthesis, QSAR and Calcium Channel Antagonist Activity of New 1,4-Dihydropyridine Derivatives Containing 1-Methyl-4,5-dichloroimidazolyl Substituents. [J] . Hosseini M, Miri R, Amini M, Archiv der Pharmazie . 2007,第10期

机译：含1-甲基-4,5-二氯咪唑基取代基的新型1,4-二氢吡啶衍生物的合成，QSAR和钙通道拮抗活性。
2. Synthesis and calcium channel antagonist activity of 1,4-dihydropyridine derivatives containing 4-nitroimidazolyl substituents. [J] . Shafiee A, ms.ac.ir, Rastkary N, Arzneimittel-Forschung: =Drug Research . 2002,第7期

机译：含4-硝基咪唑基取代基的1,4-二氢吡啶衍生物的合成及其钙通道拮抗剂活性。
3. Synthesis and calcium channel antagonist activity of new 1,4-dihydropyridine derivatives containing dichloroimidazolyl substituents. [J] . Amini Mohsen, Golabchifar AliA, Dehpour AhmadR, Arzneimittel-Forschung: =Drug Research . 2002,第1期

机译：含二氯咪唑基取代基的新1,4-二氢吡啶衍生物的合成及钙通道拮抗剂活性。
4. QSAR Analysis of 1,4-Dihydropyridine CalciumChannel Antogonists [C] . Pinar Kahraman, Metin Türkay 17th European symposium on computer aided process engineering . 2007

机译：1,4-二氢吡啶钙通道拮抗剂的QSAR分析
5. Synthesis and pharmacological activity of 1,3,6-trisubstituted-4-oxo-1,4-dihydro-quinoline-2-carboxylic acid derivatives as selective ET(A) antagonists. [D] . Patel, Hardik J. 2009

机译：1,3,6-三取代-4-氧代-1,4-二氢喹啉-2-羧酸衍生物作为选择性ET（A）拮抗剂的合成及药理活性。
6. Molecular simulations study of novel 1,4-dihydropyridines derivatives with a high selectivity for Cav3.1 calcium channel [O] . Xiaoguang Liu, Hui Yu, Xi Zhao, 2012

机译：对Cav3.1钙通道具有高选择性的新型1,4-二氢吡啶衍生物的分子模拟研究
7. Synthesis of 1,4-Dihydropyridine-5-phosphonates and Their Calcium-Antagonistic and Antihypertensive Activities. Novel Calcium-Antagonist 2-(Benzyl(phenly)amino)ethyl 5-(5,5-Dimethyl-2-oxo-1,3,2-dioxaphosphorinan-2-yl)-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3-pyridinecarboxylate Hydrochloride Ethanol(NZ-105) and Its Crystal Structure. [O] . Ryozo SAKODA, Yoshimasa KAMIKAWAJI, Kiyotomo SETO 1992

机译：1,4-二氢吡啶-5-膦酸盐的合成及其钙 - 拮抗和抗高血压活性。新型钙 - 拮抗剂2-（苄基（苯）氨基）乙基5-（5,5-二甲基-2-氧代-1,3,2-二氧化磷酸二烷-2-基）-1,4-二氢-2,6-二甲基-4-（3-硝基苯基）-3-吡啶羧酸盐盐酸盐（NZ-105）及其晶体结构。

Synthesis, QSAR and Calcium Channel Antagonist Activity of New 1,4-Dihydropyridine Derivatives Containing 1-Methyl-4,5-dichloroimidazolyl Substituents.

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