107583-03-9Relevant academic research and scientific papers
An unusual polyheterocyclic diversity by the π-cyclisation of N-carbamoyliminium ion, with or without tandem N,N-acetal cleavage, from spiro(imidazolidinoquinazolinones)
Pesquet, Anthony,Daich, Adam,Coste, Servane,Van Hijfte, Luc
, p. 1389 - 1396 (2008/12/21)
Spiro(imidazolidinoquinazolinones), obtained easily in one step from 1-carbamoylisatins, are readily converted in three steps by successive N-alkylations and sodium borohydride regio-selective reduction into the corresponding hydroxyspirolactams. The latt
Biological activities and quantitative structure-activity relationships of spiro[imidazolidine-4,4'(1'H)-quinazoline]-2,2',5(3'H)-triones as aldose reductase inhibitors
Yamagishi,Yamada,Ozaki,Asao,Shimizu,Suzuki,Matsumoto,Matsuoka,Matsumoto
, p. 2085 - 2094 (2007/10/02)
A series of spiro[imidazolidine-4,4'(1'H)-quinazoline]-2,2',5(3'H)-triones were prepared and tested for aldose reductase inhibitory activity. The 6'- halogenated derivatives were found to be highly potent in vitro inhibitors of male rabbit lens aldose reductase and in vivo inhibitors of polyol accumulation in the sciatic nerves of galactosemic rats. Of these, (4R)-6'- chloro-3'-methylspiro[imidazolidine-4,4'(1'H)-quinazoline]-2,2',5(3'H)-trione (67) showed the most potent in vitro and in vivo activities. An oral dose of 3 g/kg of compound 67 caused neither death nor behavioral abnormality in the preliminary acute toxicity study using mice and rats. Compound 67 was selected as a candidate for further evaluation. The quantitative structure- activity relationships in this series are also discussed.
Quinazolin-2-ones having a spirohydantoin ring. III. A general and efficient synthesis of 3'-substituted spiro[imidazolidine-4,4'(1'H)-quinazoline]-2,2',5(3'H)-triones
Yamagishi,Ozaki,Yamada,Da-Te,Okamura,Suzuki
, p. 1694 - 1698 (2007/10/02)
The reaction of 1-carbamoylisatins 2 with 2-ethyl-2-isothiourea hydrobromide in the presence of triethylamine followed by acid-catalyzed cyclization of the resulting 4-(2-ethyl-2-isothioureido)carbonyl-3,4-dihydro-4-hydroxy-2(1H)- quinazolinones provides
