Synthesis and biological activity of 1-acetyl-2,3-diaryl-1, 2,3,4-tetrahydroquinazoline-4-ones

Chemical modification of the alkaloid 2,3-tetramethylene-3,4-dihydroquinazol-4-one

“…Under similar conditions, 3 was acylated by 4-nitrobenzoylchloride to give 1-(4-nitrobenzoyl)-2,3-tetramethylene-1,2,3,4-tetrahydroquinazol-4-one (7).…”

“…Acylation of 2-aryl-3H-(benzyl, aryl)-1,2,3,4-tetrahydroquinazol-4-ones by acetic or trifluoroacetic anhydrides and adamantylcarboxylic and acetic acid chlorides is known to give the N-1 acyl derivatives [7]. Acylation of other simple 1,2,3,4-tetrahydroquinazol-4-ones has not been reported.…”

Introductory Chapter: The Newest Research in Quinazolinone and Quinazoline Derivatives

“…and has antimalarial activity, 100 times greater than quinine. This compound has not found clinical application, since it is 300 times toxic than quinine alkaloids [4,9,10,21] (Figure 1).…”

“…The high activity and small toxicity of methaqualone were a motivation for study of the large number of its analogues [9] (Figure 2).…”

“…Introduction of chlorine in position seven and sulfamide group in position six of quinazolines-4 brings the high active diuretics and saluretics of the chlorothiazide type. Diuretic action of the substances increases when they are turning from quinazolones-4 to tetrahydroquinazolones [9].…”