{Reference Type}: Journal Article
{Title}: Identification of sulfonylpyrimidines as novel selective aldosterone synthase (CYP11B2) inhibitors.
{Author}: Meguro M;Miyauchi S;Kanao-Arisumi Y;Naito S;Suzuki K;Inoue S;Yamada K;Homma T;Chiba K;Nara F;Furuzono S;
{Journal}: Bioorg Med Chem
{Volume}: 108
{Issue}: 0
{Year}: 2024 Jun 15
{Factor}: 3.461
{DOI}: 10.1016/j.bmc.2024.117775
{Abstract}: 4-[(5-[2-Methyl-5-(methylsulfonyl)pentan-2-yl]sulfonylpyrimidin-4-yl)amino]benzonitrile 2 was identified as a novel potent aldosterone synthase inhibitor. Compound 2 was found to inhibit human CYP11B2 in the nanomolar range, and showed an aldosterone-lowering effect in a furosemide-treated cynomolgus monkey model. Although human CYP11B2 has the high homology sequence with human CYP11B1, compound 2 showed more than 80 times higher selectivity over human CYP11B1 in vitro.