1,2,4-Thiadiazole acyclic nucleoside phosphonates as inhibitors of cysteine dependent enzymes cathepsin K and GSK-3β

0538783 - ÚOCHB 2022 RIV GB eng J - Journal Article
Pomeislová, Alice - Otmar, Miroslav - Rubešová, Petra - Benýšek, Jakub - Matoušová, Marika - Mertlíková-Kaiserová, Helena - Pohl, Radek - Poštová Slavětínská, Lenka - Pomeisl, Karel - Krečmerová, Marcela
1,2,4-Thiadiazole acyclic nucleoside phosphonates as inhibitors of cysteine dependent enzymes cathepsin K and GSK-3β.
Bioorganic & Medicinal Chemistry. Roč. 32, Feb 15 (2021), č. článku 115998. ISSN 0968-0896. E-ISSN 1464-3391
R&D Projects: GA MŠMT(CZ) LM2018133; GA MŠMT(CZ) EF16_019/0000729
Institutional support: RVO:61388963 ; RVO:61389013 ; RVO:68378271
Keywords : thiadiazoles * 5-amino-1,2,4-thiadiazol-3-(2H)-one * acyclic nucleoside phosphonates * epigenetic * cathepsin K * glycogen synthase kinase 3β
OECD category: Biochemistry and molecular biology; Polymer science (UMCH-V); Organic chemistry (FZU-D)
Impact factor: 3.461, year: 2021
Method of publishing: Limited access
https://doi.org/10.1016/j.bmc.2021.115998

A series of 1,2,4-thiadiazol-3(2H)-ones bearing 2-phosphonomethoxyethyl (PME) and 3-hydroxy-2-(phosphonomethoxy)propyl (HPMP) group were explored as potential inhibitors of ¬ human cathepsin K and glycogen synthase kinase 3β. Several compounds exhibited an inhibitory activity in the low micromolar range. The inhibitory potency of some of them toward GSK-3β was similar to tideglusib.
Permanent Link: http://hdl.handle.net/11104/0316958