Davey D D, Erhardt P W, Cantor E H, Greenberg S S, Ingebretsen W R, Wiggins J
Department of Medicinal Chemistry, Berlex Laboratories, Inc., Cedar Knolls, New Jersey 07927.
J Med Chem. 1991 Sep;34(9):2671-7. doi: 10.1021/jm00113a002.
A series of novel imidazoquinoxalinones and their aza analogues were prepared by the cyclization of o-amino(1H-imidazol-1-yl)aryls and heteroaryls with carbonyldiimidazole. The compounds were screened for inhibition of Type I and Type IV phosphodiesterases (PDE's) and evaluated for their vasorelaxant and positive inotropic activities in vitro. In general, compounds having potent PDE inhibitory activity also possessed good inotropic and vasodilator activity, although linear correlations between these activities could not be established.
通过邻氨基（1H-咪唑-1-基）芳基和杂芳基与羰基二咪唑环化反应制备了一系列新型咪唑并喹喔啉酮及其氮杂类似物。对这些化合物进行了I型和IV型磷酸二酯酶（PDE）抑制活性筛选，并在体外评估了它们的血管舒张和正性肌力活性。总体而言，具有强效PDE抑制活性的化合物也具有良好的正性肌力和血管舒张活性，尽管这些活性之间无法建立线性相关性。
