- Facile synthetic approach towards vasorelaxant active 4-hydroxyquinazoline-4-carboxamides
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A Facile synthetic approach is reported towards 4-hydroxyquinazoline-4-carboxamides 13a-i through ring expansion of 2,3-dioxoindoline-1-carboxamides 10a-c during secondary amine 11a-d nucleophilic reaction. Single crystal X-ray studies of 10c and 13d supp
- Aziz, Marian N.,Panda, Siva S.,Shalaby, Elsayed M.,Fawzy, Nehmedo G.,Girgis, Adel S.
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- Eco-friendly chemoselective N-functionalization of isatins mediated by supported KF in 2-MeTHF
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A sustainable, efficient method for the chemoselective N-functionalization of isatins based on the use of KF-Celite in 2-methyltetrahydrofuran is reported. Notably, the protocol allows reactions with a wide range of electrophiles such as alkyl halides, is
- Mamuye, Ashenafi Damtew,Monticelli, Serena,Castoldi, Laura,Holzer, Wolfgang,Pace, Vittorio
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supporting information
p. 4194 - 4197
(2015/08/11)
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- An unusual polyheterocyclic diversity by the π-cyclisation of N-carbamoyliminium ion, with or without tandem N,N-acetal cleavage, from spiro(imidazolidinoquinazolinones)
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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
- Pesquet, Anthony,Daich, Adam,Coste, Servane,Van Hijfte, Luc
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p. 1389 - 1396
(2008/12/21)
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- 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
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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.
- Yamagishi,Yamada,Ozaki,Asao,Shimizu,Suzuki,Matsumoto,Matsuoka,Matsumoto
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p. 2085 - 2094
(2007/10/02)
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