114010-96-7Relevant academic research and scientific papers
PYRAZOLE MAGL INHIBITORS
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Paragraph 00231, (2018/12/13)
Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of monoacylglycerol lipase (MAGL). Furthermore, the subject compounds and compositions are useful for the treatment of pain.
PYRAZOLE COMPOUNDS AND METHODS OF MAKING AND USING SAME
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Paragraph 00306, (2017/06/12)
Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of MAGL and/or ABHD6. Furthermore, the subject compounds and compositions are useful for the treatment of, for example, pain.
PROCASPASE-ACTIVATING COMPOUNDS AND COMPOSITIONS
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Paragraph 0088; 0115-0116, (2013/04/24)
The invention provides compounds and compositions useful for the modulation of certain enzymes. The compounds and compositions can induce of cell death, particularly cancer cell death. The invention also provides methods for the synthesis and use of the compounds and compositions, including the use of compounds and compositions in therapy for the treatment of cancer and selective induction of apoptosis in cells.
Multistep continuous-flow synthesis in medicinal chemistry: Discovery and preliminary structure-activity relationships of CCR8 ligands
Petersen, Trine P.,Mirsharghi, Sahar,Rummel, Pia C.,Thiele, Stefanie,Rosenkilde, Mette M.,Ritzén, Andreas,Ulven, Trond
supporting information, p. 9343 - 9350 (2013/07/26)
A three-step continuous-flow synthesis system and its application to the assembly of a new series of chemokine receptor ligands directly from commercial building blocks is reported. No scavenger columns or solvent switches are necessary to recover the desired test compounds, which were obtained in overall yields of 49-94 %. The system is modular and flexible, and the individual steps of the sequence can be interchanged with similar outcome, extending the scope of the chemistry. Biological evaluation confirmed activity on the chemokine CCR8 receptor and provided initial structure-activity-relationship (SAR) information for this new ligand series, with the most potent member displaying full agonist activity with single-digit nanomolar potency. To the best of our knowledge, this represents the first published example of efficient use of multistep flow synthesis combined with biological testing and SAR studies in medicinal chemistry. Copyright
Inhibition of noroviruses by piperazine derivatives
Dou, Dengfeng,He, Guijia,Mandadapu, Sivakoteswara Rao,Aravapalli, Sridhar,Kim, Yunjeong,Chang, Kyeong-Ok,Groutas, William C.
supporting information; experimental part, p. 377 - 379 (2012/02/16)
There is currently an unmet need for the development of small-molecule therapeutics for norovirus infection. The piperazine scaffold, a privileged structure embodied in many pharmacological agents, was used to synthesize an array of structurally-diverse derivatives which were screened for anti-norovius activity in a cell-based replicon system. The studies described herein demonstrate for the first time that functionalized piperazine derivatives possess anti-norovirus activity. Furthermore, these studies have led to the identification of two promising compounds (6a and 9l) that can be used as a launching pad for the optimization of potency, cytotoxicity, and drug-like characteristics.
