Abstract:
:The design, synthesis, and capacity to inhibit HIF prolyl 4-hydroxylases (PHDs) are described for 2-[2-(3-hydroxy-pyridin-2-yl)-thiazol-4-yl]-acetamide analogs. These analogs revealed two kinds of novel scaffolds as PHD2 inhibitors. Synthetic routes were developed for the preparation of their analogs containing the new scaffolds. In addition, the structure-activity relationship (SAR) of the 2-[2-(3-hydroxy-pyridin-2-yl)-thiazol-4-yl]-acetamide derivatives and their biological activities were reported. The complex structure of compound 18 with PHD2 was also obtained for the purpose of more efficient lead optimization.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Hong YR,Kim HT,Ro S,Cho JM,Lee SH,Kim IS,Jung YHdoi
10.1016/j.bmcl.2014.05.003subject
Has Abstractpub_date
2014-07-15 00:00:00pages
3142-5issue
14eissn
0960-894Xissn
1464-3405pii
S0960-894X(14)00490-9journal_volume
24pub_type
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