26033-23-8Relevant academic research and scientific papers
Synthesis and evaluation of antimicrobial and anticancer activities of 3-phenyl-1-phenylsulfonyl pyrazoles containing an aminoguanidine moiety
Huang, Yushan,Hu, Hongmei,Yan, Rui,Lin, Liwen,Song, Mingxia,Yao, Xiaodong
, (2020/10/15)
A series of 3-phenyl-1-phenylsulfonyl pyrazoles containing an aminoguanidine moiety was designed, synthesized, and evaluated for their antimicrobial and anticancer activities. The majority of the target compounds showed broad-spectrum antimicrobial activi
Synthesis and biological evaluation of some pyrazole derivatives, containing (Thio) semicarbazide, as dual anti-inflammatory antimicrobial agents
Liang, Zhaochang,Huang, Yuping,Wang, Shiben,Deng, Xianqing
, p. 1020 - 1030 (2019/10/28)
Background: Several series of pyrazole derivatives containing (thio) semicarbazide (4a-4h, 5a-5l, 6a-6f, 7a-7c) were designed and synthesized to screen dual inflammatory and antimicrobial activities. Methods: The products were characterized by1
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.
Structure-activity relationship study of a novel necroptosis inhibitor, necrostatin-7
Zheng, Weihong,Degterev, Alexei,Hsu, Emily,Yuan, Junying,Yuan, Chengye
scheme or table, p. 4932 - 4935 (2009/05/26)
Necroptosis is a regulated caspase-independent cell death mechanism characterized by morphological features resembling non-regulated necrosis. Necrotatin-7 (Nec-7), a novel potent small-molecule inhibitor of necroptosis, is structurally distinct from previously described necrostatins (Nec-1, Nec-3, Nec-4 and Nec-5). Here, we describe a series of structural modifications and the structure-activity relationship (SAR) of the Nec-7 series for inhibiting necroptosis.
Synthesis of 3-substituted arylpyrazole-4-carboxylic acids
Lebedev,Lebedeva,Sheludyakov,Kovaleva,Ustinova,Kozhevnikov
, p. 782 - 789 (2007/10/03)
A method was suggested for preparing previously unknown 3-aryl-substituted pyrazole-4-carboxylic acids, involving Vilsmeier formylation of semicarbazones of 26 available mono- and disubstituted acetophenones and 2-acetylthiophene followed by oxidation of
