Dipartimento di Scienze Farmaceutiche, University of Genoa, V.le Benedetto XV, 3-16132 Genova, Italy.
Bioorg Med Chem Lett. 2012 Jan 15;22(2):1125-9. doi: 10.1016/j.bmcl.2011.11.103. Epub 2011 Dec 3.
In pursuing our research on some 2,4-diamino-benzopyranopyrimidines and 2-amino-5,6-dihydrobenzo[h]quinazolines, previously reported as antiplatelet and analgesic/anti-inflammatory agents respectively, we designed and synthesized a new series of 5,6-dihydrobenzo[h]quinazoline 2,4-diamino substituted. The insertion of amino substituents at positions 2 and 4 of the benzoquinazoline scaffold resulted in compounds endowed with a potent ASA-like antiplatelet activity, combined with an anti-inflammatory activity comparable, in some cases, to that of indomethacin, used as a reference drug.
在研究先前报道的具有抗血小板和镇痛/抗炎作用的 2,4-二氨基苯并吡喃并嘧啶和 2-氨基-5,6-二氢苯并[h]喹唑啉时,我们设计并合成了一系列新型 5,6-二氢苯并[h]喹唑啉 2,4-二氨基取代物。在苯并喹唑啉骨架的 2 位和 4 位引入氨基取代基,得到了具有强效 ASA 样抗血小板活性的化合物,同时具有抗炎活性,在某些情况下与作为参比药物的吲哚美辛相当。