40261-59-4Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of 1, 3-disubstituted-pyrazole derivatives as new class i and IIb histone deacetylase inhibitors
Yao, Yiwu,Liao, Chenzhong,Li, Zheng,Wang, Zhen,Sun, Qiao,Liu, Chunping,Yang, Yang,Tu, Zhengchao,Jiang, Sheng
supporting information, p. 639 - 652 (2015/02/19)
A novel series of HDAC inhibitors demonstrating class I and IIb subtype selectivity have been identified using a scaffold-hopping strategy. Several designed compounds showed better selectivity for class I and IIb over class IIa HDAC isoforms comparing to the FDA approved HDAC targeting drug SAHA. A representative lead compound 22 bearing a biphenyl moiety demonstrated promising class I and IIb HDAC isoforms selectivity and in vitro anticancer activities against several cancer cell lines. This work could serve as a fundamental platform for further exploration of selective HDAC inhibitors using designed molecular scaffold.
Discovery and optimization of substituted 1-(1-phenyl-1H-pyrazol-3-yl) methanamines as potent and efficacious type II calcimimetics
Poon, Steve F.,St Jean Jr., David J.,Harrington, Paul E.,Henley III, Charles,Davis, James,Morony, Sean,Lott, Fred D.,Reagan, Jeff D.,Lu, Jenny Ying-Lin,Yang, Yuhua,Fotsch, Christopher
supporting information; experimental part, p. 6535 - 6538 (2010/04/03)
Our efforts to discover potent, orally bioavailable type II calcimimetic agents for the treatment of secondary hyperparathyroidism focused on the development of ring constrained analogues of the known calcimimetic R-568. The structure-activity relationships of various substituted heterocycles and their effects on the human calcium-sensing receptor are discussed. Pyrazole 15 was shown to be efficacious in a rat in vivo pharmacodynamic model.
NOVEL COMPOUNDS AS AGONIST FOR PPAR GAMMA AND PPAR ALPHA, METHOD FOR PREPARATION OF THE SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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Page/Page column 141, (2010/02/11)
The present invention relates to novel compounds accelerating the activity of Peroxisome proliferator-activated receptor gamma (PPARγ) and alpha (PPARα), processes of preparing the same, and pharmaceutical compositions containing the same as an active agent.
ν-Triazolines, XXIV-Pyrazolecarbaldehydes from 5-Amino-4,5-dihydro-4-methylene-ν-triazoles and Sydnones
Destro, Riccardo,Erba, Emanuela,Forti, Luciana,Pocar, Donato,Scarcella, Daniela
, p. 1377 - 1388 (2007/10/02)
The sydnones 1a-c react with the 4,5-dihydro-ν-triazoles 2a-c by long refluxing at 110-140 deg C affording via non-isolable adducts with elimination of CO2 and N2 and rearrangement a mixture of 4,5-dihydropyrazoles 3a-c, 3-pyrazolecarbaldehyde anils 4a-d, and 3-pyrazolecarbaldehydes 5a-c.Compounds 3 can be deaminated to give 4 which can be hydrolyzed to yield the 3-pyrazolecarbaldehydes 5. - The sydnones 6a,b react similarey with 2a to give a mixture of 4-pyrazolecarbaldehyde anils 7a,b and 4-pyrazolecarbaldehydes 8a,b.The structural assignments are based on spectroscopic and X-ray diffraction data.
