In vivo anti-inflammatory activity and docking study of newly synthesized benzimidazole derivatives bearing oxadiazole and morpholine rings

Rathore, Ankita; Sudhakar, Raja; Ahsan, Mohamed Jawed; Ali, Abuzer; Subbarao, Naidu; Jadav, Surender Singh; Umar, Sadiq; Yar, Mohammad Shahar

doi:10.1016/j.bioorg.2016.11.014

Cited by 64 publications

(36 citation statements)

References 39 publications

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“…The 13 C NMR spectra of these compounds displayed signals originated from C-4 and C- The synthesis of 1,2,4-triazole (23) was carried out from the intramolecular cyclisation of thioamide 21 in the basic media. The reaction was carried out in water as a non-toxic solvent under thermal, microwave and ultrasonic conditions.…”

Section: Resultsmentioning

confidence: 99%

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Synthesis of Thiazole Derivatives as Antimicrobial Agents by Green Chemistry Techniques

Demirci¹

2018

Journal of the Turkish Chemical Society Section A: Chemistry

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Amines (2) and (26) were obtained from the condensation of the corresponding amines with 3,4-difluoronitrobenzene. The reduction of nitro group produced the corresponding amines (3 and 27). The synthesis of esters (7, 12, 19, 28) was carried out from the treatment of the amines, (1, 3, 18, 27) with ethyl bromoacetate, then these compounds were converted to the corresponding hydrazides (8, 13, 29) by the treatment with hydrazine hydrate. The triazole was obtained from the intramolecular cyclisation of the corresponding carbothioamide in basic media and this compound was then converted to the morpholine-triazole-penicillin hybrid by a mannich reaction. The cyclocondensation of hydrazine carbothioamides (9b, 14, 21) or urea (4) with 2-bromo-1-(4-chlorophenyl)ethenone generated the thiazole derivatives. On the other hand, the treatment of 4, 9b, and 14 with ethyl bromoacetate yielded 4-oxo-1,3thiazolidines (6, 11, 16). Three methods containing conventional, microwave, and ultrasoundmediated techniques were applied. Best results were assessed using microwave-and ultrasoundpromoted procedures. The structures of the newly synthesised compounds were elucidated by spectroscopic techniques, and the antimicrobial activity screening studies were also performed. Some of them exhibited good to moderate activity on the test bacteria.

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Section: Resultsmentioning

confidence: 99%

“…FT-IR spectra were recorded using a Perkin Elmer 1600 series FTIR spectrometer. 1 H NMR and 13 C NMR spectra were recorded in DMSO-d6 on a BRUKER AVENE II 400 MHz NMR Spectrometer…”

Section: Sonication Technique Constitutes Another Methodology Which Smentioning

confidence: 99%

Synthesis of Thiazole Derivatives as Antimicrobial Agents by Green Chemistry Techniques

Demirci¹

2018

Journal of the Turkish Chemical Society Section A: Chemistry

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“…21 Bioactive molecules containing the oxadiazole ring have increasingly been discovered and studied over the last few years ( Figure 6). 22 It is possible to find the oxadiazole group in various molecules with reported activity as antitumor, 23 antioxidant, 24 antibacterial, 25 antiviral, 26 antiinflammatory, 27 insecticidal 28 and antiparasitic 29 agents, for example.…”

Section: Nitrogen Heterocycles and Drug Discoverymentioning

confidence: 99%

1,2,4- and 1,3,4-Oxadiazoles as Scaffolds in the Development of Antiparasitic Agents

Pitasse-Santos¹,

Sueth-Santiago²,

Lima³

2017

J. Braz. Chem. Soc.

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In this review, we present the potential use of the heterocyclic oxadiazole rings in the design and synthesis of new drugs to treat parasitic infections. We intend to compare herein all the four isomeric forms of oxadiazole rings as well as discuss the differences and similarities between them. In addition, we discuss aspects on their reactivity that justify the great importance of both 1,2,4-and 1,3,4-oxadiazoles isomers when compared with their other two isomers. Although some oxadiazole isomers satisfy Hückel's rule, there are differences concerning their aromaticity, which have a great impact on the possible interactions of the oxadiazole ring with biological receptors. The set of works selected from the literature and discussed herein points out the oxadiazole core as an important and versatile scaffold in the development of new chemical entities potentially useful as antiparasitic drugs.

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“…To overcome the MDR limitations many research has taken place and in that oxadiazole is one of the promising scaffold in the medicinal chemistry [2]. Oxadiazoles are physiologically active heterocyclic compounds owing to a vast sphere of biological activities, including anticancer [3][4][5][6][7][8][9][10][11], antidiabetic [12], antiviral [13,14], anti-inflammatory [15,16], antibacterial [17,18], antifungal [19], antimycobacterial [20], analgesic [21], anticonvulsant [22], tyrokinase inhibitor [23] and cathepsin K inhibitor [24] antioxidant [25] properties.…”

Section: Introduction and Experimentalmentioning

confidence: 99%

Synthesis, characterisation and evaluation of oxadiazole as promising anticancer agent

2020

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A unique series oxadiazoles were synthesized by cyclization of benzophenone hydrazide, followed by the nucleophillic alkylation of heterocyclic scaffold. Synthesized title compounds were characterized by the FT-IR, LCMS and NMR spectral techniques. The newly synthesized compounds were screened for the anticancer activity. IC 50 values of the 7h observed for in-vitro anti-cancer activities were 112.6 µg/ml and 126.7 µg/ml, against the MCF-7 and KB cell lines respectively. Most active compounds were found to be less toxic, which were determined by MTT assay method with normal cell line (L292). Biological screening of the synthesized series of compounds reveals that, Compound 7h was the potent molecule.Electronic supplementary material The online version of this article (https ://doi.org/10.1007/s4245 2-020-2511-z) contains supplementary material, which is available to authorized users. * S. V. Mamatha, mamatha.zh32@yahoo.com |

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In vivo anti-inflammatory activity and docking study of newly synthesized benzimidazole derivatives bearing oxadiazole and morpholine rings

Cited by 64 publications

References 39 publications

Synthesis of Thiazole Derivatives as Antimicrobial Agents by Green Chemistry Techniques

Synthesis of Thiazole Derivatives as Antimicrobial Agents by Green Chemistry Techniques

1,2,4- and 1,3,4-Oxadiazoles as Scaffolds in the Development of Antiparasitic Agents

Synthesis, characterisation and evaluation of oxadiazole as promising anticancer agent

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