Discovery of MK-8318, a Potent and Selective CRTh2 Receptor Antagonist for the Treatment of Asthma

[Image: see text] A novel series of tricyclic tetrahydroquinolines were identified as potent and selective CRTh2 receptor antagonists. The agonism and antagonism switch was achieved through structure-based drug design (SBDD) using a CRTh2 receptor homologue model. The challenge of very low exposures...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Huang, Xianhai, Brubaker, Jason, Zhou, Wei, Biju, Purakkattle J., Xiao, Li, Shao, Ning, Huang, Ying, Dong, Li, Liu, Zhidan, Bitar, Rema, Buevich, Alexei, Jung, Joon, Peterson, Scott L., Butcher, John W., Close, Joshua, Martinez, Michelle, MacCoss, Rachel N., Zhang, Hongjun, Crawford, Scott, McCormick, Kevin D., Aslanian, Robert, Nargund, Ravi, Correll, Craig, Gervais, Francois, Qiu, Hongchen, Yang, Xiaoxin, Garlisi, Charles, Rindgen, Diane, Maloney, Kevin M., Siliphaivanh, Phieng, Palani, Anandan
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2018
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6047040/
https://ncbi.nlm.nih.gov/pubmed/30034600
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.8b00145
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