Quinoline-based imidazole-fused heterocycles as new inhibitors of 15-lipoxygenase

被引：16

作者：

Dianat, Shima ^{[1
]}

Moghimi, Setareh ^{[2
,3
]}

Mahdavi, Mohammad ^{[4
]}

Nadri, Hamid ^{[5
]}

Moradi, Alireza ^{[5
]}

Firoozpour, Loghman ^{[4
]}

Emami, Saeed ^{[6
,7
]}

Mouradzadegun, Arash ^{[1
]}

Shafiee, Abbas ^{[2
,3
]}

Foroumadi, Alireza ^{[2
,3
,4
]}

机构：

[1] Shahid Chamran Univ, Dept Chem, Fac Sci, Ahvaz, Iran

[2] Univ Tehran Med Sci, Fac Pharm, Dept Med Chem, Tehran, Iran

[3] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran, Iran

[4] Univ Tehran Med Sci, Drug Design & Dev Res Ctr, Tehran, Iran

[5] Shahid Sadoughi Univ Med Sci, Fac Pharm, Dept Med Chem, Yazd, Iran

[6] Mazandaran Univ Med Sci, Fac Pharm, Dept Med Chem, Sari, Iran

[7] Mazandaran Univ Med Sci, Fac Pharm, Pharmaceut Sci Res Ctr, Sari, Iran

来源：

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | 2016年 / 31卷

基金：

美国国家科学基金会;

关键词：

Docking study; enzyme inhibitors; 15-lipoxygenase; imidazo[1; 2-a]pyridine; imidazo[2; 1-b]thiazole; POTENT INHIBITORS; 5-LIPOXYGENASE; 12/15-LIPOXYGENASE; ATHEROSCLEROSIS; DERIVATIVES; DOCKING;

D O I：

10.1080/14756366.2016.1206087

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of 2-chloro-quinoline-based imidazopyridines 6a-l and imidazothiazoles 6m-o bearing a bulky alkylamine side chain were synthesized as soybean 15-LOX inhibitors. The target compounds 6a-o were prepared via one-pot reaction of 2-chloroquinoline-3-carbaldehyde (3), heteroaromatic amidine 4, and alkyl isocyanides 5, in the presence of NH4Cl. All compounds showed significant anti-15-LOX activity (IC50 values40M). Among the title compounds, the imidazo[2,1-b]thiazole derivative 6n bearing a tert-butylamine moiety showed the highest activity against soybean 15-LOX enzyme.

引用

页码：205 / 209

页数：5

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