136353-19-0Relevant academic research and scientific papers
Rapid abnormal [3+2]-cycloaddition of isatinN,N′-cyclic azomethine imine 1,3-dipoles with chalcones
Yue, Guizhou,Dou, Zhengjie,Zhou, Zexi,Zhang, Li,Feng, Juhua,Chen, Huabao,Yin, Zhongqiong,Song, Xu,Liang, Xiaoxia,Wang, Xianxiang,Rao, Hanbing,Lu, Cuifen
supporting information, p. 8813 - 8817 (2020/06/08)
The rapid synthesis of novel dicyclic spiropyrrolidine was reported, using [3+2]-cycloaddition of isatinN,N′-cyclic azomethine imine 1,3-dipoles, generated from the condensation of substituted isatins and pyrazolidones, with chalcones in 2-5 min. The dicy
Studies of NMR Chemical Shifts of Chalcone Derivatives of Five-membered Monoheterocycles and Determination of Aromaticity Indices
Jeong, Eun Jeong,Lee, In-Sook Han
, p. 668 - 673 (2019/07/12)
A series of the chalcone derivatives of the five-membered monoheterocyclic compounds, (E)-1-aryl-3-heteroarylpropen-1-ones, were prepared by aldol condensation of the corresponding aldehydes of thiophene, pyrrole, and furan with m- and p-substituted acetophenones. Similar condensation of the acetyl compounds of the heterocycles with m- and p-substituted benzaldehydes gave another series of the chalcone derivatives, (E)-1-heteroaryl-3-arylpropen-1-ones. The 13C chemical shift values (δC) of the chalcone derivatives were determined in order to find if they correlated with the Hammett σ values. A good correlation, especially for the β-C for both series, was found for the 13C chemical shift values (δC) of the chalcone derivatives with the Hammett σ values. The chemical shift values of the β-C of the heterocyclic compounds were plotted against those of the benzene derivatives. The resulting slopes were found to be close to the values of the aromaticity indices.
Effect of solvent polarity on the photophysical properties of chalcone derivatives
Kumari, Rekha,Varghese, Anitha,George, Louis,Sudhakar
, p. 24204 - 24214 (2017/07/11)
The absorption and fluorescence characteristics of (E)-3-(furan-2-yl)-1-(4-nitrophenyl)prop-2-en-1-one (FNPO), (E)-1-(4-aminophenyl)-3-(furan-2-yl)prop-2-en-1-one (AFPO) and (E)-3-(furan-2-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one (FHPO) were recorded in eig
Synthesis, cyclooxygenase inhibition and anti-inflammatory evaluation of new 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives possessing methanesulphonyl pharmacophore
Abdellatif, Khaled R. A.,Elsaady, Mohammed T.,Abdel-Aziz, Salah A.,Abusabaa, Ahmed H. A.
, p. 1545 - 1555 (2016/10/09)
A new series of 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives 13a–p were synthesized via aldol condensation of 3/4-nitroacetophenones with appropriately substituted aldehydes followed by cyclization of the formed chalcones with 4-methanesulfonylphenylhydrazine hydrochloride. All the synthesized compounds were evaluated for their cyclooxygenase (COX) inhibition, anti-inflammatory activity and ulcerogenic liability. All compounds were more potent inhibitors for COX-2 than COX-1. While most compounds showed good anti-inflammatory activity, compounds 13d, 13f, 13k and 13o were the most potent derivatives (ED50 = 66.5, 73.4, 79.8 and 70.5 μmol/kg, respectively) in comparison with celecoxib (ED50 = 68.1 μmol/kg). Compounds 13d, 13f, 13k and 13o (ulcer index = 3.89, 4.86, 4.96 and 3.92, respectively) were 4–6 folds less ulcerogenic than aspirin (ulcer index = 22.75) and showed approximately ulceration effect similar to celecoxib (ulcer index = 3.35). In addition, molecular docking studies were performed for compounds 13d, 13f, 13k and 13o inside COX-2 active site which showed acceptable binding interactions (affinity in kcal/mol ?2.1774, ?6.9498) in comparison with celecoxib (affinity in kcal/mol ?6.5330).
Synthesis and anti-inflammatory evaluation of new 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives possessing an aminosulphonyl pharmacophore
Abdellatif, Khaled R. A.,Abdelgawad, Mohamed A.,Elshemy, Heba A. H.,Alsayed, Shahinda S. R.,Kamel, Gehan
, p. 1932 - 1942 (2015/11/24)
A novel series of 2-pyrazoline derivatives 13a-l was synthesized via aldol condensation of 4-substituted acetophenones with appropriately substituted aldehydes followed by cyclization of the formed chalcones with 4-hydrazinobenzenesulfonamide hydrochlorid
Iron-catalyzed aerobic oxidative aromatization of 1,3,5-trisubstituted pyrazolines
Ananthnag, Guddekoppa S.,Adhikari, Adithya,Balakrishna, Maravanji S.
, p. 240 - 243 (2013/12/04)
A simple and high yielding method for the synthesis of tri-substituted pyrazoles via iron(III) catalyzed aerobic oxidative aromatization of pyrazolines has been reported. The process demonstrates a variety of functional group tolerance.
Chalcones as promising pesticidal agents against diamondback moth (Plutella xylostella): Microwave-assisted synthesis and structure-activity relationship
Kumar, Rakesh,Sharma, Prabha,Shard, Amit,Tewary, Dhananjay Kumar,Nadda, Gireesh,Sinha, Arun Kumar
experimental part, p. 922 - 931 (2012/08/14)
A series of chalcones (A-CH=CH-CO-B) were synthesized under microwave irradiation, and for the first time their pesticidal activity against diamondback moth (Plutella xylostella) was evaluated to identify the promising lead structures. The structure-activity relationship (SAR) analysis revealed that electron-withdrawing substituents on ring A of chalcone provided good pesticidal agents, whereas, ring B can bear either electron-withdrawing or electron-releasing substituents. Moreover, compound 22 having para-Cl substitution on ring A as well on ring B showed maximum activity with LC 50 value of 170.24 μg mL-1. Springer Science+Business Media, LLC 2011.
Synthesis and anti-bacterial activity of some heterocyclic chalcone derivatives bearing thiofuran, furan, and quinoline moieties
Zheng, Chang-Ji,Jiang, Sheng-Ming,Chen, Zhen-Hua,Ye, Bai-Jun,Piao, Hu-Ri
experimental part, p. 689 - 695 (2012/06/01)
36 Novel heterocyclic chalcone derivatives were synthesized and tested for their anti-bacterial activity. Some compounds presented good anti-microbial activities against Gram-positive bacteria (including the multidrug-resistant clinical isolates). This cl
Design, synthesis, and bioactivities screening of a diaryl ketone-inspired pesticide molecular library as derived from natural products
Zhang, Hong,Jin, Hong,Ji, Lan-Zhu,Tao, Ke,Liu, Wei,Zhao, Hao-Yu,Hou, Tai-Ping
experimental part, p. 94 - 100 (2012/06/01)
Three natural products, 1,5-diphenylpentan-1-one, 1,5-diphenylpent-2-en-1-one, and 3-hydroxy-1,5-diphenylpentan-1-one, with good insecticidal activities were extracted from Stellera chamaejasme L. Based on their shared diaryl ketone moiety as 'pharmacophores', a series of diaryl ketones were synthesized and tested for insecticidal activity, acetylcholinesterase inhibitory activity, and antifungal activity. All synthesized compounds showed poor insecticidal and acetylcholinesterase inhibitory activities. Compound III with a furyl ring showed strong activities against plant pathogenic fungi. The IC50 of compound (E)-1-(2,4-dichlorophenyl)-3-(furan-2-yl)- -prop-2-en-1-one (III2) was 1.20mg/L against Rhizoctonia solani, suggesting its strong potential as a novel antifungal drug.
