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Identification of the minimum PAR4 inhibitor pharmacophore and optimization of a series of 2-methoxy-6-arylimidazo[2,1-b][1,3,4]thiadiazoles

This letter describes the further deconstruction of the known PAR4 inhibitor chemotypes (MWs 490 – 525 and with high plasma protein binding) to identify a minimum PAR4 pharmacophore devoid of metabolic liabilities and improved properties. This exercise identified a greatly simplified 2-methoxy-6-ary...

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Publicat a:Bioorg Med Chem Lett
Autors principals: Temple, Kayla J., Duvernay, Matthew T., Maeng, Jae G., Blobaum, Anna L., Stauffer, Shaun R., Hamm, Heidi E., Lindsley, Craig W.
Format: Artigo
Idioma:Inglês
Publicat: 2016
Matèries:
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC5340293/
https://ncbi.nlm.nih.gov/pubmed/27777004
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2016.10.020
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