92210-39-4Relevant academic research and scientific papers
Synthesis and Cardiotonic Activity of a Series of Substituted 4-Alkyl-2(1H)-quinazolinones
Bandurco, Victor T.,Schwender, Charles F.,Bell, Stanley C.,Combs, Donald W.,Kanojia, Ramesh M.,et al.
, p. 1421 - 1426 (2007/10/02)
The synthesis, cardiac fraction III cyclic nucleotide phosphodiesterase (PDE-III) inhibition, and positive inotropic activity of a series of 2(1H)-quinazolinones are reported.A general synthesis of the series involved the cyclization of 2-aminoacetophenones with potassium cyanate in acetic acid.Modifications at the 4-position of the quinazoline nucleus were best achieved by formation of the intermediate N1-acyl-N3-phenylurea from the substituted phenyl isocyanate and appropriate carboxamide.PPA was used to ring close to the quinazoline product.Generally the SAR for the series paralleled the five-point model previously published for PDE-III inhibition.The most active analogue of the series was 5,6-dimethoxy-4-methyl-2(1H)-quinazolinone (1) (ORF 16600), which had about twice the intravenous potency of amrinone.Compound 1 is currently under development as an orally active cardiotonic.
5,6-Dialkoxy-3,4-optionally substituted-2(1H)quinazolinones, composition and method of use
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, (2008/06/13)
The synthesis of substituted quinazolinones is described. The novel quinazolinones are renal vasodilators and thereby increase renal blood flow, and are useful as cardiovascular agents.
