Synthesis of new 5,6-dihydrobenzo[h]quinazoline 2,4-diamino substituted and antiplatelet/antiphlogistic activities evaluation
作者:Chiara Brullo、Massimo Rocca、Paola Fossa、Elena Cichero、Elisabetta Barocelli、Vigilio Ballabeni、Lisa Flammini、Carmine Giorgio、Francesca Saccani、Giuseppe Domenichini、Olga Bruno
DOI:10.1016/j.bmcl.2011.11.103
日期:2012.1
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
在继续研究以前分别报道为抗血小板药和镇痛/抗炎药的2,4-二氨基-苯并吡喃并嘧啶和2-氨基-5,6-二氢苯并[ h ]喹唑啉的过程中,我们设计并合成了一系列新的5被6-6-二氢苯并[ h ]喹唑啉2,4-二氨基取代。在苯并喹唑啉骨架的2和4位上插入氨基取代基导致化合物具有强大的ASA样抗血小板活性,并且在某些情况下还具有与消炎痛类似的消炎活性,作为参比药物。