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Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639
[Image: see text] The discovery of a novel peripherally acting and selective Ca(v)3.2 T-type calcium channel blocker, ABT-639, is described. HTS hits 1 and 2, which have poor metabolic stability, were optimized to obtain 4, which has improved stability and oral bioavailability. Modification of 4 to...
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| Publicado no: | ACS Med Chem Lett |
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| Main Authors: | , , , , |
| Formato: | Artigo |
| Idioma: | Inglês |
| Publicado em: |
American Chemical
Society
2015
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| Acesso em linha: | https://ncbi.nlm.nih.gov/pmc/articles/PMC4468402/ https://ncbi.nlm.nih.gov/pubmed/26101566 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00023 |
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