Inhibitors of lipoprotein(a) assembly

Autor:	Randy Ramharack, Peggy Liao, Janak Khimchand Padia, Bruce D. Roth, Patt William Chester, Helen Tsenwhei Lee, Mark A Spahr, Jason K. Pontrello, Karen Elaine Sexton, Mark A. Massa
Rok vydání:	2003
Předmět:	Stereochemistry Clinical Biochemistry Pharmaceutical Science Mice Transgenic Pharmacology Biochemistry Chemical synthesis Cell Line Inhibitory Concentration 50 Mice Structure-Activity Relationship In vivo Oral administration Drug Discovery Animals Humans Structure–activity relationship Amino Acids Molecular Biology chemistry.chemical_classification Sulfonamides Dose-Response Relationship Drug biology Chemistry Organic Chemistry Haplorhini Lipoprotein(a) Amino acid Dose–response relationship biology.protein Molecular Medicine Lipoprotein
Zdroj:	Bioorganic & Medicinal Chemistry. 11:4827-4845
ISSN:	0968-0896
DOI:	10.1016/j.bmc.2002.04.001
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a8eb8e08ad1868ff21ba683a1dd33e9 https://doi.org/10.1016/j.bmc.2002.04.001 Zobrazit plný text záznamu Full Text from ScienceDirect