13982-55-3Relevant academic research and scientific papers
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.
Synthesis, characterization, and antioxidant activity of some new benzodiazepine derivatives
Bhat, K. Ishwar,Kumar, Abhishek
, p. 397 - 400 (2018/09/29)
A series of novel 4-(substituted phenyl)-2-(2-thienyl)-2,3-dihydro-1H-benzo[b] [1,4] diazepines (MB1-MB8) has been synthesized from 3-(substituted phenyl)-1-(2-thienyl)prop-2-en-1ones (MC1-MC8). The latter compo
Inhibitory potential of some chalcones on cathepsins B, H and L
Garg, Shweta,Raghav, Neera
, p. 72937 - 72949 (2015/09/15)
Cathepsins, intracellular proteases, are known to be involved in a number of physiological processes such as degradation of extracellular proteins, prohormone processing, progressions of atherosclerosis etc. High levels of cathepsins have also been indica
Antioxidant and antimicrobial studies on fused-ring pyrazolones and isoxazolones
Mazimba, Ofentse,Wale, Kabo,Loeto, Daniel,Kwape, Tebogo
, p. 6564 - 6569 (2015/02/19)
A series of 3-nitrochalcones have been synthesized enroute towards fused ring pyrazolones and isoxazolones. Base catalyzed condensation of the chalcones with ethylacetoacetate yielded cyclohexenones in good yields (74-76%). The treatment of cyclohexenones with hydrazine hydrate or hydroxylamine chloride in the presence of a base afforded the corresponding fused-ring pyrazolinones (70-78% yield) and isoxazolinones (58-66% yield). The newly synthesized compounds were characterized by IR, 1D and 2D NMR and HRMS spectral analysis. The compounds were screened for their antioxidant and antimicrobial activities. Pyrazolinones showed good DPPH radical scavenging and iron metal chelating properties. The para-hydroxy group was important for a compound to have enhanced antioxidant activity. Pyrazolinones and isoxazolinone exhibited a wider range of antimicrobial activities compared to cyclohexenones. Pyrazolinones and isoxazolinone bearing a thiophene ring were the most potent type of compounds against Bacillus subtilis and Candida albicans with MIC values of 0.313-1.25 μg/mL. Some of the synthesized compounds were found to have promising antioxidant, metal chelation and antimicrobial activities.
Synthesis, pharmacological, and biological screening of novel derivatives of benzodiazepines
Bhat, K. Ishwar,Chauhan, Manoj Kumar Singh,Kumar, Abhishek,Kumar, Pankaj
, p. 1189 - 1192 (2014/08/05)
A series of novel 4-(substituted phenyl)-2-(thiophen-2-yl)-2,3-dihydro-1H- benzo[b][1,4]diazepine have been synthesized from 3-(substituted phenyl)-1-(thiophen-2-yl)prop-2-en-1-one. 3-(Substituted phenyl)-1-(thiophen-2- yl)prop-2-en-1-one was prepared by
Synthesis and antibacterial activity of some heterocyclic chalcone analogues alone and in combination with antibiotics
Tran, Thanh-Dao,Nguyen, Thi-Thao-Nhu,Do, Tuong-Ha,Huynh, Thi-Ngoc-Phuong,Tran, Cat-Dong,Thai, Khac-Minh
experimental part, p. 6684 - 6696 (2012/08/28)
A series of simple heterocyclic chalcone analogues have been synthesized by Claisen Schmidt condensation reactions between substituted benzaldehydes and heteroaryl methyl ketones and evaluated for their antibacterial activity. The structures of the synthe
A new and direct synthesis of chalcones via TFAA-H3PO 4 mediated c-c bond forming reaction
Kankanala, Kavitha,Reddy, Lingam Venkata,Reddy, Vangala Ranga,Mukkantia, Khagga,Pal, Sarbani
scheme or table, p. 53 - 59 (2012/04/18)
A number of α,β-unsaturated carboxylic acids were reacted with electron rich arenes or heteroarene in the presence of trifluoroacetic anhydride (TFAA) and H3PO4 at room temperature to give a variety of chalcone derivatives in good to
Synthesis of 3,5-disubstituted isoxazolines and isoxazoles
Ingle,Doshi,Raut,Kadu
body text, p. 1815 - 1818 (2012/06/15)
2-Acetylthiophene condenses with different aromatic aldehyde in ethanol in the presence of aqueous NaOH to give 1-(2′thienyl)-3-(substituted phenyl)-2-propen-1-one(Ia-e) which reacts with hydroxylamine hydrochloride and aqueous KOH in presence of ethonal medium to give 3-(2′-thienyl)-5- (substituted phenyl)-2-isoxazoline (IIa-e). And 3-(2′-thienyl)- 5-(substituted phenyl)-Δ2-isoxazoline (IIa-e) was dissolved in DMSO. To this catalytic amount of iodine was added. Cooled and diluted with water. The solid thus separated was washed with 20% sodium thiosulphate to give 3-(2′-thienyl)-5-(substituted phenyl)-isoxazole (II′a-e). Characterization and structural elucidation were done on the basis of melting points determination, analytical and spectral studies.
Synthesis of 3,5-disubstituted pyrazoles and their derivatives
Ingle,Doshi,Raut,Kadu
scheme or table, p. 1691 - 1698 (2012/06/15)
2-Acetylthiophene condenses with different aromatic aldehyde in ethanol in the presence of aqueous NaOH to give 1-(2′-thienyl)-3-(substituted phenyl)-2-propen-1-one (Ia-e) which reacts with hydrazine hydrate in ethanol to give pyrazoline (IIa-e) and also treated with DMSO in presence of catalytic amount of iodine to give pyrazole (II′a-e) Similarly, 1-phenyl pyrazoline (IIIa-e) treated with DMSO/I2 to give 1-phenyl pyrazole(III′a- e), 1-(2,4-dinitro phenyl) pyrazoline (IVa-e) treated with DMSO/I2 to give 1-(2,4-dinitro phenyl) pyrazole(IV′a-e), 1-carboxamido pyrazoline (Va-e) treated with DMSO/I2 to give 1-carboxamido pyrazole (V′a-e), 1-acetyl pyrazoline (VIa-e) treated with DMSO/I2 to give 1-acetyl pyrazole (VI′a-e), 1-benzoyl pyrazoline (VIIa-e) treated with DMSO/I2 to give 1-benzoyl pyrazole (VII′a-e) and 1-nitroso pyrazoline (VIIIa-e) treated with DMSO/I2 to give 1-nitroso pyrazole (VIII′a-e). Characterization and structural elucidation was carried out on the basis of melting points determination, analytical and spectral studies.
Synthesis of thiophen-2-yl pyrimidines as antitumor, analgesic and antiinflammatory agents
James, Jainey P.,Bhat, Ishwar K.
, p. 309 - 312 (2013/09/24)
A series of novel thiophen-2-yl pyrimidine derivatives IV, V(a-e) have beenf synthesized from the intermediate chalcones III(a-h). The structures of these compounds were confirmed by IR, NMR, Mass spectroscopy and elemental analysis. Biological studies of
