35344-95-7Relevant articles and documents
Polymorphs of a pyrazole nitronyl nitroxide and its complexes with metal(ii) hexafluoroacetylacetonates
Catala, Laure,Wurst, Klaus,Amabilino, David B.,Veciana, Jaume
, p. 2736 - 2745 (2006)
The synthesis of pyrazol-4-yl nitronyl nitroxide is reported, along with the crystal structures of its polymorphs and coordination compounds with nickel(ii) and cobalt(ii) hexafluoroacetylacetonate. The polymorphic forms of the pure radical show very different magnetic properties: the alpha form shows only antiferromagnetic interactions while those of the beta form reveal competing ferro- and anti-ferromagnetic interactions. This phenomenon can be traced to the relative orientations of the spin carriers in the crystal. These, in turn, are determined in large measure by the hydrogen bonding networks, where a competition between [N-H...O] and [N-H...N] hydrogen bonds is observed. This delicate balance is also seen in the coordination chemistry of the radical acting as a ligand for the hexafluoroacetylacetonate complexes of nickel(ii) and cobalt(ii). In the former, a 2 1 radical metal complex is formed because of coordination of the pyrazolyl nitrogen atom only. In the latter, a cyclic dimer is formed which involves both the nitrogen and oxygen as coordinating atoms. In both cases, the NH groups of the pyrazolyl moiety lead to the formation of hydrogen bonded networks in the crystals. The magnetic properties of the complexes reveal antiferromagnetic interactions. However, the pyrazolyl nitronyl nitroxide has been proven an interesting component for the formation of coordination compounds with hydrogen bonds in between the magnetic components. The Royal Society of Chemistry 2006.
CEREBLON BINDERS FOR THE DEGRADATION OF IKAROS
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Page/Page column 318; 319, (2019/10/23)
The present invention provides cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway along with their use in therapeutic applications as described herein.
Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors
Zhang, Han,Liu, Huan,Luo, Xiao,Wang, Yuxi,Liu, Yuan,Jin, Hongwei,Liu, Zhenming,Yang, Wei,Yu, Peilin,Zhang, Liangren,Zhang, Lihe
, p. 235 - 252 (2018/05/09)
Transient receptor potential melastatin 2 (TRPM2), a Ca2+-permeable cationic channel, plays critical roles in insulin release, cytokine production, body temperature regulation and cell death as a reactive oxygen species (ROS) and temperature sensor. However, few TRPM2 inhibitors have been reported, especially TRP-subtype selective inhibitors, which hampers the investigation and validation of TRPM2 as a drug target. To discover novel TRPM2 inhibitors, 3D similarity-based virtual screening method was employed, by which 2,3-dihydroquinazolin-4(1H)-one derivative H1 was identified as a TRPM2 inhibitor. A series of novel 2,3-dihydroquinazolin-4(1H)-one derivatives were subsequently synthesized and characterized. Their inhibitory activities against the TRPM2 channel were evaluated by calcium imaging and electrophysiology approaches. Some of the compounds exhibited significant inhibitory activity, especially D9 which showed an IC50 of 3.7 μM against TRPM2 and did not affect the TRPM8 channel. The summarized structure-activity relationship (SAR) provides valuable insights for further development of specific TRPM2 targeted inhibitors.
