Discovery of a potent nicotinic Acid receptor agonist for the treatment of dyslipidemia.
ACS Med Chem Lett
; 2(2): 171-6, 2011 Feb 10.
Article
en En
| MEDLINE
| ID: mdl-24900295
ABSTRACT
Nicotinic acid has been used clinically for decades to control serum lipoproteins. Nicotinic acid lowers very low-density lipoprotein (VLDL)-cholesterol, low-density lipoprotein (LDL)-cholesterol, and lipoprotein-a (LPa), and it is also effective in raising high-density lipoprotein (HDL)-cholesterol. However, nicotinic acid has several side effects in clinical use. The most notable is intense cutaneous vasodilation "flushing" on the upper body and face. We discovered a pyranopyrimidinedione series to be nicotinic acid receptor agonists. A potent nicotinic acid receptor agonist from this series {5-(3-cyclopropylpropyl)-2-(difluoromethyl)-3H-pyrano[2,3-d]pyrimidine-4,7-dione}with reduced flushing side effect in dogs was identified.
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01-internacional
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MEDLINE
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En
Revista:
ACS Med Chem Lett
Año:
2011
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Article