Department of Medicinal Chemistry, Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India.
Bioorg Med Chem Lett. 2013 Feb 15;23(4):1104-9. doi: 10.1016/j.bmcl.2012.11.121. Epub 2012 Dec 8.
Substituted 1,4-dihydropyridines were discovered as a novel and potent series of phosphodiesterase 4 (PDE4) inhibitors. Structure-activity relationships within this series have been carried out and studies revealed that the dihydropyridine core, with indole moiety and 3,4-dimethoxybenzyl group, is a potent analogue for PDE4 inhibition. These novel series of compounds were prepared via a 3-component reaction in a single pot. In vitro biological activity, modeling studies and crystallography data are also reported.
取代的 1,4-二氢吡啶被发现是一种新型且有效的磷酸二酯酶 4（PDE4）抑制剂系列。在该系列中进行了结构-活性关系的研究，研究表明二氢吡啶核心、吲哚部分和 3,4-二甲氧基苄基是 PDE4 抑制的有效类似物。这些新型化合物系列是通过一锅法的 3 组分反应制备的。还报告了体外生物活性、建模研究和晶体学数据。
