Discovery of SCH 900271, a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia

[Image: see text] Structure-guided optimization of a series of C-5 alkyl substituents led to the discovery of a potent nicotinic acid receptor agonist SCH 900271 (33) with an EC(50) of 2 nM in the hu-GPR109a assay. Compound 33 demonstrated good oral bioavailability in all species. Compound 33 exhibi...

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Hlavní autoři: Palani, Anandan, Rao, Ashwin U., Chen, Xiao, Huang, Xianhai, Su, Jing, Tang, Haiqun, Huang, Ying, Qin, Jun, Xiao, Dong, Degrado, Sylvia, Sofolarides, Michael, Zhu, Xiaohong, Liu, Zhidan, McKittrick, Brian, Zhou, Wei, Aslanian, Robert, Greenlee, William J., Senior, Mary, Cheewatrakoolpong, Boonlert, Zhang, Hongtao, Farley, Constance, Cook, John, Kurowski, Stan, Li, Qiu, van Heek, Margaret, Wang, Gangfeng, Hsieh, Yunsheng, Li, Fangbiao, Greenfeder, Scott, Chintala, Madhu
Médium: Artigo
Jazyk:Inglês
Vydáno: American Chemical Society 2011
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC4025820/
https://ncbi.nlm.nih.gov/pubmed/24900372
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml200243g
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