新型三唑和曼尼希碱官能化的1,4-二氢吡啶作为血管紧张素转换酶（ACE）抑制剂的合成与评价
Synthesis and evaluation of novel triazoles and mannich bases functionalized 1,4-dihydropyridine as angiotensin converting enzyme (ACE) inhibitors.
作者信息
Kumbhare Ravindra M, Kosurkar Umesh B, Bagul Pankaj K, Kanwal Abhinav, Appalanaidu K, Dadmal Tulshiram L, Banerjee Sanjay Kumar
机构信息
Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500607, India.
Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500607, India.
出版信息
Bioorg Med Chem. 2014 Nov 1;22(21):5824-30. doi: 10.1016/j.bmc.2014.09.027. Epub 2014 Sep 19.
A series of novel diethyl 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate embedded triazole and mannich bases were synthesized, and evaluated for their angiotensin converting enzyme (ACE) inhibitory activity. Screening of above synthesized compounds for ACE inhibition showed that triazoles functionalized compounds have better ACE inhibitory activity compared to that of mannich bases analogues. Among all triazoles we found 6 h, 6 i and 6 j to have good ACE inhibition activity with IC50 values 0.713 μM, 0.409 μM and 0.653 μM, respectively. Among mannich bases series compounds, only 7c resulted as most active ACE inhibitor with IC50 value of 0.928 μM.
合成了一系列新型的2,6-二甲基-1,4-二氢吡啶-3,5-二羧酸二乙酯嵌入三唑和曼尼希碱，并对其血管紧张素转换酶（ACE）抑制活性进行了评估。对上述合成化合物进行ACE抑制筛选表明，与曼尼希碱类似物相比，三唑官能化化合物具有更好的ACE抑制活性。在所有三唑中，我们发现6h、6i和6j具有良好的ACE抑制活性，IC50值分别为0.713μM、0.409μM和0.653μM。在曼尼希碱系列化合物中，只有7c是活性最高的ACE抑制剂，IC50值为0.928μM。
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