1028296-78-7Relevant academic research and scientific papers
Pyridopyrimidine Angiotensin II Antagonists
Ellingboe, John W.,Antane, Madelene,Nguyen, Thomas T.,Collini, Michael D.,Antane, Schuyler,et al.
, p. 542 - 550 (2007/10/02)
A series of pyridopyrimidine angiotensin II (A II) antagonists was synthesized and tested for antagonism of A II. Compounds with a biphenyltetrazole pharmacophore and small alkyl groups at the 2- and 4-positions of the pyridopyrimidine ring were found to be the most potent in an AT1 receptor binding assay and in blocking the A II pressor response in anesthetized, ganglion-blocked A II-infused rats. 5,8-Dihydro-2,4-dimethyl-8--4-yl)methyl>pyridopyrimidin-7(6H)-one (4a) was one of the more potent compounds in the binding assay and was the most efficacious compound in the A II-infused rat model. Further study of 4a in Goldblatt (2K-1C) rats showed the compound to have oral bioavailability and to be an efficacious and potent compound in a high renin form of hypertension.
