2492-30-0Relevant articles and documents
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
Aminopyrimidine compound, composition containing same and application thereof
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Paragraph 0122; 0125; 0140; 0141, (2019/01/06)
The invention discloses an aminopyrimidine compound as shown in a formula (I), preparation and application thereof, and particularly discloses an aminopyrimidine compound as shown in the formula (I),or polymorphism, pharmaceutically acceptable salt, prodr
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.
New approach towards the synthesis of selenosemicarbazones, useful compounds for Chagas' disease
Pizzo, Chiara,Faral-Tello, Paula,Yaluff, Gloria,Serna, Elva,Torres, Susana,Vera, Ninfa,Saiz, Cecilia,Robello, Carlos,Mahler, Graciela
, p. 107 - 113 (2016/01/15)
Herein, we describe a new approach towards the synthesis of selenosemicarbazones. The reaction involves an O-Se exchange of semicarbazones using Ishihara reagent. Eleven selenosemicarbazones were prepared using this methodology, with low to moderate yields. Among the prepared compounds the m-bromo phenyl methyl derivative 1b was selected to be evaluated in vivo, in a murine model of acute Chagas' disease. Compound 1b 10 mg/kg bw/day reduced 50% of parasitaemia profile compared with the control group, but was less effective than Benznidazole (50 mg/kg bw/day reduced 90%) and toxic. These studies are important to guide future Chagas drug design.
Synthesis and antitubercular and antibacterial activity of some active fluorine containing quinoline–pyrazole hybrid derivatives
Nayak, Nagabhushana,Ramprasad, Jurupula,Dalimba, Udayakumar
, p. 59 - 68 (2017/11/28)
In an attempt to develop newer antitubercular and antibacterial agents against the increasing bacterial resistance, we have designed new quinoline–pyrazole analogs (8a–u) following the molecular hybridization approach. The structure of one of the final compounds, 8a was unambiguously confirmed by single crystal X-ray diffraction (SC-XRD) analysis. The target compounds were evaluated for their antitubercular activity against Mycobacterium tuberculosis and antibacterial activity against three common pathogenic bacterial strains. Four derivatives (8b, 8c, 8j and 8o) displayed significant antitubercular activity. The compounds derived from 8-trifluoromethylquinoline and 6-fluoroquinoline scaffolds with halogen substitution on the pyrazole ring exhibited superior inhibition activity than corresponding 6-methoxyquinoline analogs. The cytotoxic studies revealed that the active compounds are nontoxic to normal Vero cell lines with selectivity index values ≥10, which indicate the suitability of these compounds for further drug development. The in silico molecular docking study demonstrated strong binding affinity of the compounds with the target enzymes (InhA, CYP121 and TMPK) of M. tuberculosis. Further, the in vitro antibacterial activity of compounds 8b, 8c, 8d and 8g is comparable with that of the reference drug, Ciprofloxacin.
Preparation of 2-Arylethynylselanylacetonitriles from 4-Aryl-1,2,3-selenadiazoles
O'Connor,Sachinvala,Ganjian
, p. 1167 - 1169 (2015/08/06)
Base decomposition of 4-(substituted phenyl)-1,2,3-selenadiazoles at room temperature resulted in 2-(substituted phenyl)-ethynylselenolate anions, which were immediately reacted with bromoacetonitrile to give a series of 2-(substituted phenyl)ethynylselan
Structural diversity and properties of M(II) phenyl substituted pyrazole carboxylate complexes with 0D-, 1D-, 2D- and 3D frameworks
Gong, Yunnan,Liu, Chongbo,Wen, Huiliang,Yan, Liushui,Xiong, Zhiqiang,Ding, Liang
scheme or table, p. 865 - 875 (2011/06/22)
Eight new metal complexes with two kinds of phenyl substituted pyrazole carboxylic acid, [Ni(HL1)2(H2O)2] (1), [Cu(HL1)2(H2O)2] (2), [Zn(HL1)2] (3), [Ni(HL2)2(H 2O)2] (4), [Ni(HL2)2(HL 3)2] (5), [Cu(HL2)2]·2H 2O (6), [Zn(HL2)2] (7), [Zn2(HL 2)2(L2)] (8) [H2L1 = 5-phenyl-1H-pyrazole-3-carboxylic acid; H2L2 = 3-phenyl-1H-pyrazole-4-carboxylic acid; HL3 = 3-phenyl-1H-pyrazole] were prepared by hydro/solvothermal reactions and structurally characterized. Complexes 1 and 2 have monomeric structures; 3 and 4 exhibit 1-D zig-zag chains; 5 and 6 possess 2D layer structures consisting of rhomboid grids; 7 features a 2-fold interpenetrated 3-D diamondoid framework; while complex 8 holds a 3-D NaCl-like framework. Hydrogen bonding and aromatic π-π stacking interactions link the eight complexes into 2-D (1-3) or 3-D (4-8) supramolecular networks, of which 5, 6 and 8 contain single, single and double-stranded helical chains, respectively. The thermal stabilities of complexes 1-8 and photophysical properties of complexes 3 and 7 were investigated.
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.
Basic alumina as an efficient catalyst for preparation of semicarbazones in solvent free conditions
Kiasat, Ali Reza,Kazemi, Foad,Mehrjardi, Mehdi Fallah
, p. 1337 - 1339 (2008/03/13)
An efficient and simple procedure for conversion of different classes of aldehydes and ketones into the corresponding semicarbazones with semicarbazide hydrochloride using basic alumina is studied.
