AM1 theoretical study, synthesis and biological evaluation of some benzofuran analogues of anti-inflammatory arylalkanoic acids

Santana, Lourdes; Teijeira, Marta; Uriarte, Eugenio; Terán, Carmen; Liñares, Belen; Villar, Rosa; Laguna, Reyes; Cano, Ernesto

doi:10.1016/s0928-0987(98)00019-0

Cited by 47 publications

(30 citation statements)

References 8 publications

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“…They have potent pesticidal and insecticidal [6], antitumor [7], anthelmintic [8], nematocidal [8], antifungal [9], and anti-inflammatory [10] activities. They were also found to be useful as anticonvulsant and antidepressant [11] agents and cardiac phosphodiesterase inhibitors [12].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Anticonvulsant, and Anti‐inflammatory Activities of Some New Benzofuran‐Based Heterocycles

Dawood¹,

Abdel‐Gawad

Ellithey

et al. 2006

Archiv der Pharmazie

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Treatment of 2-bromoacetylbenzofuran (2) with pyridine afforded its corresponding pyridinium bromide 3. The latter salt reacted with some activated alkenes and acetylenes to give the corresponding indolizine derivatives. Treatment of the salt 3 with benzylidenemalononitriles 9 afforded polysubstituted aniline derivatives, however with arylidenecyanothioacetamides 15 it gave the corresponding 4,5-dihydrothiophenes. Bromide 3 also coupled with p-chlorobenzenediazonium salt followed by ammonium acetate to give the corresponding 1,2,4,5-tetrazine derivative. The biological activity of the newly synthesized compounds was examined and some of them were found to possess anticonvulsant and anti-inflammatory activities.

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Section: Introductionmentioning

confidence: 99%

Synthesis, Anticonvulsant, and Anti‐inflammatory Activities of Some New Benzofuran‐Based Heterocycles

Dawood¹,

Abdel‐Gawad

Ellithey

et al. 2006

Archiv der Pharmazie

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“…Numerous synthesized benzofuran derivatives were found to be biologically active [7][8][9]. Nowadays, many synthetic benzofurans are used as good inhibitor [10,11], antimicrobial [12][13][14], anti-inflammatory [15,16], antiviral [17], antioxidant [18][19][20][21], antitumor [22], antiproliferative [23,24], and antialzheimer [25].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Aryl (5-Substituted Benzofuran-2-Yl) Carbamate Derivatives as Antimicrobial Agents

Budhwani¹,

Sharma²,

Kalyane³

2017

Asian J Pharm Clin Res

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Objectives: Benzofurans are very interesting heterocycles, which are available in nature and show a wide range of pharmacological activities, viz., antifungal, antibacterial, antitumor, antimalarial and antioxidant activity. Methods:A convenient method for the preparation of aryl (5-substituted benzofuran-2-yl) carbamate derivatives 6a-6j has been developed. The target compounds 1-(5-nitrobenzofuran-2-yl)-3-arylurea (6a-6e) and 1-(5-bromobenzofuran-2-yl)-3arylurea (6f-6j) have been prepared by reacting 5-nitrobenzofuran-2-carbonyl azide 5a or 5-bromobenzofuran-2-carbonyl azide 5b with substituted phenols in reasonable overall yields. All the synthesized compounds were characterized using Fourier transform infrared (FTIR), 1 H NMR and mass spectrometry and were subjected to antimicrobial screening against two Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis), two Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa), and two fungi (Candida albicans and Aspergillus niger) using two-fold dilution method. Results and Discussion:All the values of FTIR, 1 H NMR and mass spectra were found to be prominent. The results indicate that synthesized compound 6i showed potent antimicrobial activity comparable to standard. Conclusion:The detailed synthesis, spectroscopic data, and antimicrobial activities of synthesized compounds were reported.

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“…In nature's collection of biologically active molecules, benzofuran derivatives constitute a major group [7][8][9]. Benzofuran ring systems bearing substitutions at the C-2 position are widely distributed in nature and have been reported to have antioxidant, antiviral, antifungal activities [10,11], antimicrobial [12,13], anti-inflammatory [14], antipsychotic [15], analgesic [16], antilipidemic [17] and CNS stimulant activities [18]. Investigation of benzofuran derivatives in search of new drugs or to increase the efficacy of the present drugs has been most frequent approach [19].…”

Section: Introductionmentioning

confidence: 99%

In Vitro Antioxidant, Antimicrobial and Admet Study of Novel Furan/Benzofuran C-2 Coupled Quinoline Hybrids

Anantacharya

Satyanarayan

Patil

et al. 2017

Int J Pharm Pharm Sci

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Objective: Synthesis of novel 2-(benzofuran-2-yl) and 2-(furan-2-yl) quinoline-4-carboxylates and their [2-(1-benzofuran-2-yl) quinolin-4-yl] methanol, [2-(1-furan-2-yl) quinolin-4-yl] methanol and its derivatives for antioxidant, antimicrobial and in silico pharmacokinetic study.Methods: Synthesis was carried with the conventional method and the structures were confirmed by IR, 1 H NMR, 13 C NMR and mass spectral analysis. The antioxidant activity was performed by DPPH and H2O2 radical scavenging method. The antimicrobial investigation was established by cup plate and food poison technique. The in silico absorption, distribution, metabolism, excretion and toxicity (ADMET) study of the drug was carried out in ACD/lab-2. Results:The antioxidant activity results revealed that compounds 4b-c, 5a-b, 10c and 10f exhibited good DPPH radical and hydrogen peroxide scavenging activity. The antibacterial results revealed that compounds 4c, 5a-b, 10b, 10d and 10f exhibited good activity against Escherichia coli, Klebsiella pneumonia and Salmonella typhimurium. Further, the antifungal activity results showed that compounds 4c, 5c and 10c-e were showing good activity against Aspergillusflavus and Candida neoformans. The mean value of P<0.05 were considered to be statistically significant. The ADMET results revealed that compounds emerged as a potential candidate for antioxidant and antimicrobial agents. Conclusion:The study reveals that compounds containing furan/benzofuran coupled heterocycles played the important role for activity as they possess potent antioxidant and antimicrobial agents. The in silico ADME analysis also suggesting the compounds were in acceptable range to obey the pharmacokinetic parameters.

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AM1 theoretical study, synthesis and biological evaluation of some benzofuran analogues of anti-inflammatory arylalkanoic acids

Cited by 47 publications

References 8 publications

Synthesis, Anticonvulsant, and Anti‐inflammatory Activities of Some New Benzofuran‐Based Heterocycles

Synthesis, Anticonvulsant, and Anti‐inflammatory Activities of Some New Benzofuran‐Based Heterocycles

Synthesis of Aryl (5-Substituted Benzofuran-2-Yl) Carbamate Derivatives as Antimicrobial Agents

In Vitro Antioxidant, Antimicrobial and Admet Study of Novel Furan/Benzofuran C-2 Coupled Quinoline Hybrids

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