The SAR of 6-(N-alkyl-N-acyl)-2-propyl-3-[(2′-tetrazol-5-yl)biphen-4-yl)methyl]-quinazolinones as balanced affinity antagonists of the human AT1 and AT2 receptors

Modification of the 6-N-alkyl-N-acyl groups of L-159,689, 6-(N-benzoyl-N-pentyl)-amino-2-propyl-3-[(2'-(tetrazol-5-yl)biphen-4-yl)methyl] led to the identification of the 6-(N-benzoyl-N-(3-pyridylmethyl)) analog(L-162,537). L-162,537 had improved aqueous solubility and oral bioavailability in the dog. The SAR of this class of AT(1) and AT(2) Ligands is discussed.