86293-51-8Relevant academic research and scientific papers
Antibacterial and anti-inflammatory activity of valproic acid-pyrazole conjugates as a potential agent against periodontitis
Dong, Lei,Fang, Ling,Dai, Xinxiang,Zhang, Jia,Wang, Jia,Xu, Pei
, p. 131 - 141 (2021/07/10)
Periodontitis is a serious global concern. Therefore, in the present study, we intend to synthesize novel valproic-acid pyrazole conjugates as a novel agent against periodontitis. The molecules were developed in a facile synthetic route and obtained in ex
Hydroxyl- and Halogen-containing Chalcones for the Inhibition of LPS-stimulated ROS Production in RAW 264.7 Macrophages: Design, Synthesis and Structure–Activity Relationship Study
Shrestha, Aarajana,Shrestha, Aastha,Park, Pil-Hoon,Lee, Eung-Seok
, p. 729 - 734 (2019/07/19)
Oxidative stress due to overproduction of reactive oxygen species (ROS) plays a major role in inflammation, cancer, and neurodegenerative disorders. In this study, 60 chalcone derivatives with fluorine (F), trifluoromethyl (CF3), trifluoromethoxy (OCF3), chlorine (Cl), and bromine (Br) in ring A and with or without hydroxy (OH) in ring B were designed, synthesized, and screened for inhibitory activity against lipopolysaccharide (LPS)-stimulated ROS production in RAW 264.7 macrophages. Structure–activity relationship study revealed the importance of a hydroxyl moiety in ring B for enhancing inhibitory activity of ROS production. Furthermore, a hydroxyl group at the ortho-position is more essential for inhibition of ROS production followed by meta- and para-positions. Among all, compound 27 that contains para-chlorine moiety in ring A and ortho-hydroxy in ring B displayed the strongest inhibitory activity (IC50 = 3.42 μM) against LPS-stimulated ROS production in RAW264.7 macrophages.
Microwave-assisted synthesis and bioevaluation of new sulfonamides
Gul, Halise Inci,Yamali, Cem,Yesilyurt, Fatma,Sakagami, Hiroshi,Kucukoglu, Kaan,Gulcin, Ilhami,Gul, Mustafa,Supuran, Claudiu T.
, p. 369 - 374 (2017/11/10)
In this study, 4-[5-(4-hydroxyphenyl)-3-aryl-4,5-dihydro-1H-pyrazol-1-yl]benzenesulfonamide derivatives (8-14) were synthesized for the first time by microwave irradiation and their chemical structures were confirmed by 1H NMR, 13C N
A Green, Solvent-Free, Microwave-Assisted, High-Yielding YbCl3Catalyzed Deprotection of THP/MOM/Ac/Ts Ethers of Chalcone Epoxide and 2′-Aminochalcone and Their Sequel Cyclization
Kumar, Sumit,Verma, Nishant,Parveen, Iram,Ahmed, Naseem
supporting information, p. 2111 - 2122 (2016/11/23)
Under microwave and solvent-free conditions, YbCl3efficiently catalyzed the deprotection of tetrahydropyran-2-yl, methoxymethyl (MOM), acetyl, and tosyl groups and sequel cyclization of chalcone epoxide to 2-hydroxyindanone and 2′-aminochalcone to aza-flavanone. The reaction afforded the products in excellent yield (78–99%) at 850 W microwave heating within 1–5 min under eco-friendly conditions. The merits of the presented protocol include high yield, use of microwave irradiation, solvent-free condition, catalyst reusability, and no need for purification with column chromatography. The present method is very much milder but more advanced than those reported earlier.
Highly efficient deprotection of phenolic tetrahydropyranyl and methoxymethyl ethers and sequel cyclization to indanones using Sn(IV)Cl 4 catalyst
Ahmed, Naseem,Pathe, Gulab Khushalrao,Venkata Babu
supporting information, p. 3683 - 3687 (2014/06/23)
Sn(IV)Cl4 catalyst provided a rapid and efficient deprotection method for the phenolic THP and MOM ethers and sequel intramolecular Friedel-Crafts alkylation reaction of THP and MOM protected chalcone epoxides under mild conditions. The reaction took 2-3 min to give the products in excellent yield (90-98%) at 0 °C without affecting the other functional groups.
Synthesis and study of antibacterial activity of some 1-phenyl-3-aryl-5-(4- (2-ethanoloxy) phenyl)-1H-pyrazoles
Goyal, Anju,Jain, Neelam,Jain, Sandeep
, p. 553 - 558 (2013/11/06)
A series of 1-phenyl-3-aryl-5-(4-(2-ethanoloxy) phenyl)-1H-pyrazoles were synthesized from chalcones and studied for their in vitro antibacterial activity. Chalcones i.e., 1-aryl-3-(4-hydroxyphenyl) prop-2-en-1-ones, 1 on reaction with phenyl hydrazine yi
Zinc oxide as a regioselective and heterogeneous catalyst for the synthesis of chalcones at room temperature
More, Parmeshwar E.,Bandgar, Babasaheb P.,Kamble, Vinod T.
, p. 30 - 32 (2012/10/30)
Zinc oxide catalyzed synthesis of chalcones has been carried out under solvent-free conditions at room temperature. Activated as well as unactivated aromatics smoothly underwent Friedel-Crafts acylation with α, β-unsaturated acid chlorides furnishing excellent yields of the corresponding chalcones. The zinc oxide can be recovered and reused at least three times without any appreciable loss in activity.
Synthesis, molecular docking and evaluation of thiazolyl-pyrazoline derivatives as EGFR TK inhibitors and potential anticancer agents
Lv, Peng-Cheng,Li, Dong-Dong,Li, Qing-Shan,Lu, Xiang,Xiao, Zhu-Ping,Zhu, Hai-Liang
scheme or table, p. 5374 - 5377 (2011/10/12)
Fourty-two thiazolyl-pyrazoline derivatives were synthesized to screen for their EGFR kinase inhibitory activity. Compound 4-(4-chlorophenyl)-2-(3-(3,4- dimethylphenyl)-5-p-tolyl-4,5-dihydro-1H-pyrazol-1-yl)thiazole (11) displayed the most potent EGFR TK inhibitory activity with IC50 of 0.06 μM, which was comparable to the positive control. Molecular docking results indicated that compound 11 was nicely bound to the EGFR kinase. Compound 11 also showed significant antiproliferative activity against MCF-7 with IC 50 of 0.07 μM, which would be a potential anticancer agent.
Synthesis and biological activity of 4,6-substituted aryl-1-acetyl pyrimidine-2-ols
Bamnela, Rita,Shrivastava
experimental part, p. 6553 - 6558 (2010/12/25)
The synthesis of 4-(4'-bromophenyl)-6-substituted aryl-1-acetyl-pyrimidine-2-ols have been reported. The synthesized derivatives were characterized by elemental analysis and spectral data (IR and 1H NMR). All the synthesized derivatives have been evaluated for their antimicrobial and anthelmintic activities against microbes and helminthes.
Iodine-catalyzed efficient synthesis of chalcones by grinding under solvent-free conditions
Wang, Hongshe,Zeng, June
experimental part, p. 1209 - 1212 (2009/12/03)
Chalcones are useful intermediates in organic synthesis and exhibit a large number of different biological activities. Chalcones have been synthesized in high yields by Claisen-Schmidt condensation of substituted acetophenones with various aromatic aldehydes in the presence of 10 mol% of iodine at room temperature by grinding under solvent-free conditions.
