AI Article Synopsis
- - This text discusses the development of new TYK2 JH2 inhibitors, focusing on improved potency and structural differences from earlier compounds.
- - The research identified a new compound, 4h, which has been found to be a potent and selective inhibitor compared to the first-generation compound 1a.
- - The compound 4h demonstrated an hWB IC of 41 nM and showed 94% bioavailability in mouse pharmacokinetic studies, indicating its potential for effective use in further research.
Article Abstract
Efforts directed at improving potency and preparing structurally different TYK2 JH2 inhibitors from the first generation of compounds such as 1a led to the SAR study of new central pyridyl based analogs 2-4. The current SAR study resulted in the identification of 4h as a potent and selective TYK2 JH2 inhibitor with distinct structural differences from 1a. In this manuscript, the in vitro and in vivo profiles of 4h are described. The hWB IC of 4h was shown as 41 nM with 94% bioavailability in the mouse PK study.
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| http://dx.doi.org/10.1016/j.bmcl.2023.129373 | DOI Listing |
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