Compounds of the general structure A and B were investigated for their activity as lipoprotein (a),[Lp (a)], assembly (coupling) inhibitors. SAR around the amino acid derivatives (structure A) gave compound 14-6 as a potent coupling inhibitor. Oral dosing of compound 14-6 to Lp (a) transgenic mice and cymologous monkeys resulted in a> 30% decrease in plasma Lp (a) levels after 1–2 weeks of treatment at 100 mg/kg/day.
