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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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| Pubblicato in: | Bioorg Med Chem Lett |
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| Autori principali: | , , , , , , |
| Natura: | Artigo |
| Lingua: | Inglês |
| Pubblicazione: |
2016
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| Soggetti: | |
| Accesso online: | 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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