- Synthesis of benzoxazepine derivatives from pyrazole-chalcone via a simple and convenient protocol using basic alumina as solid support
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In the present study a series of novel benzoxazepine (5a-h) derivatives were synthesized by the thermal cyclization reaction of various pyrazole-chalcones (3a-h) with 2-aminophenol, by conventional heating and microwave irradiation (180 W) in solvent-free conditions in short reaction times (9-12 min), giving high yields of products (80-88%). The homogeneity of all the newly synthesized compounds has been checked by TLC. Their IR, NMR, ESI-mass spectral data and elemental analysis are in accord with the assigned structure. The title compounds were evaluated for their antibacterial activity against Gram-positive bacteria Staphylococcus aureus, Bacillus subtilis, and Gram-negative bacteria Pseudomonas aeruginosa, Escherichia coli. Compounds 3c, 3h, 5b, 5c, 5g and 5h were found to show good antibacterial activity when compared with that of standard drug Ampicillin. Furthermore, the same library of compounds were evaluated for antifungal activity against Aspergillus nigerzeae, Penicillium italicum and Fusarium oxysporum using Grieseofulvin as standard drug. The results of the above studies show that the compounds 3b, 3c, 3e, 3h, 5a, 5c, 5g and 5h showed good antifungal activity against all the tested organisms.
- Ashok,Radhika,Rao, Boddu Ananda,Sarasija,Jayashree,Sadanandam
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- Design, Synthesis, and Evaluation of Some Novel Heterocycles Bearing Pyrazole Moiety as Potential Anticancer Agents
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1,3-Diphenylpyrazole-4-carboxylaldehyde and o-hydroxyacetophenone were exploited as starting materials for the synthesis of novel substituted chalconated pyrazole derivative. The proclivity of this compound towards carbon and nitrogen nucleophiles such as malononitrile, diethyl malonate, ethyl cyanoacetate, ethyl acetoacetate, semicarbazide, thiosemicarbazide, and hydroxylamine has been investigated. The structures of all synthesized compounds were ascertained by analytical and spectral data. The antitumor activity of the target synthesized compounds was tested against a panel of two human tumor cell lines, namely, hepatocellular carcinoma (liver) HepG2 and mammary gland breast MCF-7.
- Abdelgawad, Nancy,Ismail, Mahmoud F.,Hekal, Mohamed H.,Marzouk, Magda I.
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p. 1771 - 1779
(2019/04/30)
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- Solvent free microwave assisted synthesis of Substituted 1-(3-((E)-2-(3-(aryl)-1-phenyl-1h-pyrazol-4-yl) vinyl)-benzofuran-2-yl) ethanones
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Substituted 1-(2-hydroxy phenyl)-3-[3-(4-aryl)-1-phenyl-1 H-pyrazol-4-yl]-propenones (la-h) have efficiently been synthesized by the condensation of 3-aryl-1-phenyl-pyrazole-4-carbaldehydes with 2-hydroxy acetophenones using basic alumina under solvent fr
- Ashok,Radhika
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- Synthesis and antibacterial activity of some new 2,3-dimethoxy-3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl)chromanones
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Seven new 2,3-dimethoxy-3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl)chromanones (5) have been synthesized by the oxidation of 3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl)chromones (4) with iodobenzene diacetate in methanol. The structures of compounds 5 were es
- Prakash, Om,Kumar, Rajesh,Sehrawat, Rakesh
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scheme or table
p. 1763 - 1767
(2009/06/18)
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- Synthesis and antifungal activity of some new 3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl) chromones
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Seven new 3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl) chromones 4a-g have been synthesized by the oxidation of 2-hydroxychalcone analogues of pyrazole 3a-g with hydrogen peroxide (H2O2) in KOH-MeOH by Algar Flynn Oymanda (AFO) reaction
- Prakash, Om,Kumar, Rajesh,Parkash, Vipin
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p. 435 - 440
(2008/09/18)
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