| Autor: |
Tang, Lin, Li, Minxiong, Bai, Changlin, Feng, Xuejin, Hu, Haiyang, Yao, Yufen, Li, Baiqing, Li, Hongwei, Qin, Guohong, Xi, Ning, Lv, Genpin, Zhang, Lei |
| Zdroj: |
MedChemComm; 2024, Vol. 15 Issue: 3 p856-873, 18p |
| Abstrakt: |
Three series of benzoheterocyclic-substituted amide derivatives were designed and synthesized as potent ASK1 inhibitors in this work. After undergoing continuous structural optimization, compound 17awas discovered to be a novel inhibitor of ASK1 with good potency (kinase, IC50= 26 nM), noteworthy liver microsomal stability (human, T1/2= 340.4 min), good pharmacokinetic parameters (rat, T1/2p.o. = 2.11 h, AUClastp.o. = 10 900 h ng mL−1) and high oral bioavailability (rat, F= 97.9%), while also being inactive towards hERG (IC50> 10 μM). |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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