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10.1021/ml100251u

http://scihub22266oqcxt.onion/10.1021/ml100251u
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C4017979!4017979!24900295
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suck abstract from ncbi


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pmid24900295      ACS+Med+Chem+Lett 2011 ; 2 (2): 171-6
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  • Discovery of a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia #MMPMID24900295
  • Qin J; Rao A; Chen X; Zhu X; Liu Z; Huang X; Degrado S; Huang Y; Xiao D; Aslanian R; Cheewatrakoolpong B; Zhang H; Greenfeder S; Farley C; Cook J; Kurowski S; Li Q; van Heek M; Chintala M; Wang G; Hsieh Y; Li F; Palani A
  • ACS Med Chem Lett 2011[Feb]; 2 (2): 171-6 PMID24900295show ga
  • 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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