Polycyclic N-hetero compounds. XXIII Synthesis and antidepressive activity of 4-substituted 5,6-dihydrobenzo(h)quinazolines.

Density Functional Theory Calculation of 13C NMR Shifts of Diazaphenanthrene Alkaloids: Reinvestigation of the Structure of Samoquasine A

“…Benzo[ h ]quinazoline alkaloids are a small group of natural products of varying biological activities, including antitumor and antidepressive properties. In 2000, Kobayashi and co-workers isolated an alkaloid from the seeds of the custard apple tree Annona squamosa .…”

Polycyclic N‐Heterocyclic Compounds. Part 75: Synthesis of 2,4‐Disubstituted 5,6‐dihydro[1]benzoxepino[5,4‐d]pyrimidines and 12‐Substituted 1,2,4,5‐Tetrahydro[1]benzoxepino[4,5‐e]imidazo[1,2‐c]pyrimidines as Potential Antiplatelet Aggregators

“…There are potential side effects associated with the antidepressive activity of these compounds, as seen with compounds having similar structure and antidepressive activity . During developmental research of these compounds as inhibitors of platelet aggregation, detailed pharmacological studies will need to performed, including examination of possible side effects.…”

“…We have been involved in research on the synthesis and biological evaluation of a series of polycyclic N ‐heterocyclic compounds. During our investigation of the antidepressive activity and antiplatelet aggregation activity of these compounds, we discovered that 4‐alkylamino‐5,6‐dihydrobenzo[ h ]quinazolines ( 1 ) and 4‐alkylamino‐6,7‐dihydro‐5 H ‐pyrimido[5,4‐ d ][1]benzazepines ( 2 ) had stronger inhibitory activities against collagen‐induced aggregation of rabbit platelets in vitro than aspirin, the well‐known antiplatelet agent (Figure ) . The most potent 1 (R 1 = H and R 2 = Et) had nine times the activity of aspirin, whereas the most potent 2 (NR 1 R 2 = morpholino) had 14 times the activity of aspirin.…”