1352012-63-5Relevant academic research and scientific papers
A Novel Radiotracer for Imaging Monoacylglycerol Lipase in the Brain Using Positron Emission Tomography
Wang, Changning,Placzek, Michael S.,Van De Bittner, Genevieve C.,Schroeder, Frederick A.,Hooker, Jacob M.
, p. 484 - 489 (2016)
Monoacylglycerol lipase (MAGL) is a serine hydrolase that hydrolyzes monoacylglycerols to glycerol and fatty acid and plays an important role in neuroinflammation. MAGL inhibitors are a class of molecules with therapeutic potential for human diseases of t
Discovery of novel tetrahydrobenzo[b]thiophene-3-carbonitriles as histone deacetylase inhibitors
Gediya, Piyush,Vyas, Vivek K.,Carafa, Vincenzo,Sitwala, Nikum,Della Torre, Laura,Poziello, Angelita,Kurohara, Takashi,Suzuki, Takayoshi,Sanna, Vinod,Raguraman, Varalakshmi,Suthindhiran,Ghosh, Debarpan,Bhatia, Dhiraj,Altucci, Lucia,Ghate, Manjunath D.
, (2021/03/26)
The discovery and development of isoform-selective histone deacetylase (HDAC) inhibitor is a challenging task because of the sequence homology among HDAC enzymes. In the present work, novel tetrahydro benzo[b]thiophene-3-carbonitrile based benzamides were designed, synthesized, and evaluated as HDAC inhibitors. Pharmacophore modeling was our main design strategy, and two novel series of tetrahydro benzo[b]thiophene-3-carbonitrile derivatives with piperidine linker (series 1) and piperazine linker (series 2) were identified as HDAC inhibitors. Among all the synthesised compounds, 9h with 4-(aminomethyl) piperidine linker and 14n with piperazine linker demonstrated good activity against human HDAC1 and HDAC6, respectively. Both the compounds also exhibited good antiproliferative activity against several human cancer cell lines. Both these compounds (9h and 14n) also induced cell cycle arrest and apoptosis in U937 and MDA-MB-231 cancer cells. Overall, for the first time, this research discovered potent isoform-selective HDAC inhibitors using cyclic linker instead of the aliphatic chain and aromatic ring system, which were reported in known HDAC inhibitors.
HEXAFLUOROISOPROPYL CARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
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Page/Page column 30, (2011/12/14)
The invention relates to hexafluoroisopropyl carbamate derivatives of general formula (I): wherein R, Z, A, m and n as defined in the description, in the form of the base or of an addition salt with an acid. The compounds can be used as inhibitors of the enzyme MGL (monoacyl glycerol lipase).
