7455-91-6Relevant academic research and scientific papers
Synthesis of some new quinazolin-4(3H)-one derivatives and evaluation of their anticonvulsant activity
Boshta, Nader M.,El-Essawy, Farag A.,Ammar, Ramy M.,Ismail, Abd El-Hamid,Wahba, Nancy E.
, p. 2031 - 2042 (2016/10/21)
We reported the synthesis of a novel series of quinazolin-4(3H)-one derivatives bearing oxadiazole, thiadiazole, and other moieties in the 3-position of the quinazolinone nucleus using appropriate synthetic route. The compounds were evaluated for their anticonvulsant activity using picrotoxin model, GABA-A receptor antagonist. Five compounds showed significantly prolonged times for convulsions compared with the standard drug phenobarbital. Graphical abstract: [Figure not available: see fulltext.]
THE REACTION OF QUINAZOLIN-4-ONES WITH ORGANO-METALLIC AGENTS- A PERSISTENT PREFERENCE FOR RING RUPTURE OVER CYCLIZATION
Ranganathan, Darshan,Farooqui, Firdous,Mehrotra, Sanjiv,Kesavan, Krishnan
, p. 2493 - 2506 (2007/10/02)
A range of 3-substituted quinazolin-4-ones whose conjugate bases can undergo intramolecular cyclization to tricyclic systems, have been prepared (Scheme 2).The reaction of these with a variety of organolithium agents gave products arising from reagent addition to the quinazolin-4-one 1,2 bond, although experimental results tended to demonstrate that the desired conjugate bases existed in equilibrium with the tricyclic systems.The acetyl salt of 1a with NaH gave product 3c from ring fragmentation.The imidazoquinazoline 8, the parent of which is markedly antihypotensive, resulted from endeavours to prepare a prototype of the desired tricyclic system by an alternative route.Most compounds studied have more than one site for reactivity against the reagents used.The experimental results clearly highlight an overwhelming preference for addition to quinazolin-4-one 1,2 bond.
