Synthesis of new 5,6-dihydrobenzo[h]quinazoline 2,4-diamino substituted and antiplatelet/antiphlogistic activities evaluation

  • Bioorg Med Chem Lett. 2012 Jan 15;22(2):1125-9. doi: 10.1016/j.bmcl.2011.11.103.
Chiara Brullo  1 ,  Massimo Rocca ,  Paola Fossa ,  Elena Cichero ,  Elisabetta Barocelli ,  Vigilio Ballabeni ,  Lisa Flammini ,  Carmine Giorgio ,  Francesca Saccani ,  Giuseppe Domenichini ,  Olga Bruno
Affiliations
  • 1. Dipartimento di Scienze Farmaceutiche, University of Genoa, V.le Benedetto XV, 3-16132 Genova, Italy.
PMID: 22189137 DOI: 10.1016/j.bmcl.2011.11.103
Abstract

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.