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Can I read Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors on EtoBox?
Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors by Han Zhang; Huan Liu; Xiao Luo; Yuxi Wang; Yuan Liu; Hongwei Jin; Zhenming Liu; Wei Yang; Peilin Yu; Liangren Zhang; Lihe Zhang is a Chemistry article available to read on EtoBox.
What is Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors about?
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.
Who reads Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors?
It is typically read by researchers, students, and practitioners in Chemistry.
- Author
- Han Zhang; Huan Liu; Xiao Luo; Yuxi Wang; Yuan Liu; Hongwei Jin; Zhenming Liu; Wei Yang; Peilin Yu; Liangren Zhang; Lihe Zhang
- Publisher
- Elsevier BV
- Published
- 2018
- Language
- EN
- Field
- Chemistry (Physical Sciences)