Synthesis of new 2-, 3-, and 4-substituted azidoquinolines: inhibitors of human blood platelet aggregation in vitro

Abstract A series of 2-, 3- and 4-substituted azidoquinoline derivatives were synthesized and tested for their ability to inhibit human platelet aggregation in vitro triggered by adenosine diphosphate (15 μM), collagen (5 μg/ml), platelet activating factor (10 μM), or the stable prostaglandin H 2 mimetic, U46619 (4 μM). The most active compounds (IC 50 2.5–68.3 μM) were the germinal 3,3-diazides ( 4f and 4g ) and the 4-azido-3-nitroquinolines ( 6f and 6g ).