77651-73-1Relevant academic research and scientific papers
QUINAZOLINE DERIVATIVES FOR THE TREATMENT AND PREVENTION OF DIABETES AND OBESITY
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Page/Page column 20, (2008/12/08)
The present invention relates to novel quinazoline derivatives effective in lowering blood glucose level and body weight, and a medicine for treatment and/or prevention of diabetes and/or obesity, which comprises the compound as an active ingredient.
Discovery of potent cyclic GMP phosphodiesterase inhibitors. 2-Pyridyl- and 2-imidazolylquinazolines possessing cyclic GMP phosphodiesterase and thromboxane synthesis inhibitory activities
Lee,Konishi,Yu,Miskowski,Riviello,Macina,Frierson,Kondo,Sugitani,Sircar,Blazejewski
, p. 3547 - 3557 (2007/10/03)
Moderate cyclic GMP phosphodiesterase (cGMP-PDE, PDE V) inhibitor 2- phenyl-4-anilino-quinazoline (1) was identified utilizing MultiCASE assisted drug design (MCADD) technology. Modification of compound 1 was conducted at the 2-, 4-, and 6-positions of the quinazoline ring for enhancement of cGMP- PDE inhibitory activity. The 6-substituted 2-(imidazol-1-yl)-quinazolines are 1000 times more potent in in vitro PDE V enzyme assay than the well-known inhibitor zaprinast. The 6-substituted derivatives of 2-(3- pyridyl)quinazoline 84 and 2-(imidazol-1-yl)quinazoline 86 exhibited more than 1000-fold selectivity for PDE V over the other four PDE isozymes. In addition, cGMP-PDE inhibitors 64, 65, and 73 were found to have an additional property of thromboxane synthesis inhibitory activity.
Phosphoramides. XIII. Phosphorus Pentaoxide-Amine Hydrochloride Mixtures as Reagents in the Synthesis of 4(3H)-Quinazolinones and 4-Quinazolinamines
Nielsen, Knud Erik,Pedersen, Erik B.
, p. 637 - 642 (2007/10/02)
4(3H)-Quinazolinones 3a-r have been prepared by heating methyl N-acylanthranilates 1a-c and the hydrochlorides of primary aliphatic and aromatic amines with phosphorus pentaoxide and N,N-dimethylcyclohexylamine at 180 deg C. 4-Quinazolinamines 4 and the amidine 7 were isolated as by-products.The carboxamides 5 and 6 were believed to be reaction intermediates.By raising the temperature to 250 deg C 4 was obtained in a preparative yield.
