Inhibitors of lipoprotein (a) assembly

KE Sexton, HT Lee, M Massa, J Padia, WC Patt…

Index: Sexton, Karen E.; Lee, Helen T.; Massa, Mark; Padia, Janak; Patt, William C.; Liao, Peggy; Pontrello, Jason K.; Roth, Bruce D.; Spahr, Mark A.; Ramharack, Randy Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 22 p. 4827 - 4845

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Citation Number: 7

Abstract

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.