31385-12-3Relevant articles and documents
Identification of novel quinazolin-4(3H)-ones as inhibitors of thermolysin, the prototype of the M4 family of proteinases
Khan, Mahmud Tareq Hassan,Khan, Rasool,Wuxiuer, Yimingjiang,Arfan, Mohammad,Ahmed, Manzoor,Sylte, Ingebrigt
experimental part, p. 4317 - 4327 (2010/09/12)
A combinatorial series of novel quinazolin-4(3H)-ones were synthesised and their structures were established based on spectroscopic data (IR, NMR, EI-MS, and FAB-MS). The compounds were tested for inhibition of the zinc metalloproteinase thermolysin (TLN) utilizing a chemical array-based approach. Some of the compounds were found to inhibit TLN, with IC50 values ranging from 0.0115 μM (compound 3) to 122,637 μM (compound 29). Compound 3 [3-phenyl-2-(trifluoromethyl) quinazolin-4(3H)-one] (IC50 = 0.0115 μM) and compound 35 [3-(isopropylideneamino)-2,2-dimethyl-2,3-dihydroquinazolin-4 (1H)-one] (IC50 = 0.2477 μM) were found to be the most potent inhibitors.
Aziridination of alkenes using 3-acetoxyamino-2-trifluoromethylquinazolin-4(3H)-one
Atkinson, Robert S.,Coogan, Michael P.,Cornell, Clive L.
, p. 157 - 166 (2007/10/03)
Oxidation of 3-amino-2-trifluoromethylquinazolin-4(3H)-one 6 with lead tetraacetate in dichloromethane gives the title 3-acetoxyamino derivative 7 which is isolable at room temperature and considerably more stable than the corresponding 2-alkyl substituted analogues. Compound 7 aziridinates alkenes in yields which are consistently higher than those from the 2-alkyl substituted analogues. Aziridinations using 3-acetoxyaminoquinazolinones bearing other electron-withdrawing groups on the 2-position of the quinazolinone ring have been examined.
