Design &amp; synthesis of novel oxazolone &amp; triazinone derivatives and their biological evaluation as COX-2 inhibitors

Mohamed, Lamia W.; El-Badry, Ossama M.; El‐Ansary, Afaf; Ismael, Ahmed S.

doi:10.1016/j.bioorg.2017.04.012

Cited by 24 publications

(15 citation statements)

References 18 publications

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“…Altogether,t his study established the fact that oxazolone derivatives can be investigated for the development of effective anti-inflammatory agents. [44] In 2017, Kus et al synthesised and evaluated the antioxidant potentialo fo xazole-5(4H)-one derivatives. Their work was focused on countering the oxidative cellular damaget hat leads to development of cancers, cardiovascular diseases and ageing.…”

Section: Pharmacological Profiles Of Oxazolone Derivativesmentioning

confidence: 99%

The Current Status of O‐Heterocycles: A Synthetic and Medicinal Overview

Singh

Silakari

2018

ChemMedChem

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O-Heterocycles have been explored in the field of medicinal chemistry for a long time, but their significance has not been duly recognised and they are often shunned in favour of N-heterocycles. The design of bioactive molecules for nearly every pathophysiological condition is primarily focused on novel N-heterocycles. The main reasons for such bias include the ease of synthesis and possible mimicking of physiological molecules by N-heterocycles. But considering only this criterion rarely provides breakthrough molecules for a given disease condition, and instead the risks of toxicity or side effects are increased with such molecules. On the other hand, owing to improved synthetic feasibility, O-heterocycles have established themselves as equally potent lead molecules for a wide range of pathophysiological conditions. In the last decade there have been hundreds of reports validating the fact that equally potent molecules can be designed and developed by using O-heterocycles, and these are also expected to have comparably low toxicity. Even so, researchers tend to remain biased toward the use of N-heterocycles over O-heterocycles. Thus, this review provides a critical analysis of the synthesis and medicinal attributes of O-heterocycles, such as pyrones, oxazolones, furanones, oxetanes, oxazolidinones, and dioxolonones, and others, reported in the last five years, underlining the need for and the advantages guiding researchers toward them.

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Section: Pharmacological Profiles Of Oxazolone Derivativesmentioning

confidence: 99%

The Current Status of O‐Heterocycles: A Synthetic and Medicinal Overview

Singh

Silakari

2018

ChemMedChem

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“…Of these, unsaturated oxazolones present a particular importance both for the organic synthesis, as intermediates in the obtaining of other classes of compounds, as well as for their biological properties [1,2]. A large number of derivatives from this class are reported in the literature as having biological activity, such as antitumoral [3,4], antibacterial [5][6][7][8][9][10], antifungal [5,8,9], anti-inflammatory [11], antioxidant [5,12], tyrosinase inhibitors [13,14].…”

mentioning

confidence: 99%

“…Among the heterocyclic compounds obtained from unsaturated oxazolones are the triazinones cited in the literature for different biological properties, including antitumoral [15,16], antibacterial [17][18][19], antifungal [17], antioxidant [18], anti-inflammatory [11], anticonvulsant [20].…”

mentioning

confidence: 99%

Synthesis, characterization and Cytotoxicity Evaluation of New Compounds from Oxazol-5(4H)-Ones and 1,2,4-Triazin-6(5H)-Ones Classes

Rosca¹,

Apostol²,

Drăghici³

et al. 2019

Rev. Chim.

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This paper presents the synthesis of new heterocyclic compounds from oxazoles and triazinones classes. Some 2-(4-(4-X-phenylsulfonyl)benzamido)acetic acids were condensed with 4-iodobenzaldehyde in presence of acetic anhydride and sodium acetate, when the new corresponding unsaturated oxazol-5(4H)-one were obtained. Through the reaction of these oxazol-5(4H)-ones with phenylhydrazine, in presence of the acetic acid and sodium acetate, the new heterocyclic compounds from 1,2,4-triazin-6(5H)-ones class were obtained. The structures of synthesized compounds have been confirmed by spectral methods (FT-IR, 1H-NMR, 13C-NMR and MS) and elemental analysis. The cytotoxicity of the compounds was evaluated using the Daphnia magna and Artemia salina bioassays.

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“…There are many reports that mention various oxazoles and oxazolones derivatives for their biological actions, such as antimicrobial [1][2][3], antitumoral [3][4][5], analgesic and anti-inflammatory [3,[6][7][8][9][10], including the antagonistic action upon transient receptor potential cation channel subfamily V member 1 (TRPV1) channel [11]. Moreover, there are drugs with anti-inflammatory activity containing the oxazole nucleus, being currently used in therapy.…”

Section:  Introductionmentioning

confidence: 99%

“…Moreover, there are drugs with anti-inflammatory activity containing the oxazole nucleus, being currently used in therapy. For example, oxaprozin is a non-steroidal anti-inflammatory drug with an 1,3-oxazolic nucleus that blocks prostaglandin synthesis by non-selective inhibition of both cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), that is used in the treatment of many musculoskeletal inflammatory diseases [6,12,13].…”

Section:  Introductionmentioning

confidence: 99%

New 2-(4-(4-bromophenylsulfonyl)phenyl)-4-arylidene-oxazol-5(4H)-ones: analgesic activity and histopathological assessment

Bărbuceanu

Roşca

Apostol

et al. 2020

Rom J Morphol Embryol

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This is an open-access article distributed under the terms of a Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International Public License, which permits unrestricted use, adaptation, distribution and reproduction in any medium, non-commercially, provided the new creations are licensed under identical terms as the original work and the original work is properly cited. ORIGINAL PAPER New 2-(4-(4-bromophenylsulfonyl)phenyl)-4-arylideneoxazol-5(4H)-ones: analgesic activity and histopathological assessment FLORICA BĂRBUCEANU 1,2) , ELENA-VALENTINA ROŞCA 3) , THEODORA-VENERA APOSTOL 3) , OANA-CRISTINA ŞEREMET 4) , CONSTANTIN DRĂGHICI 5) , DRAGOŞ PAUL MIHAI 4) , SIMONA NEGREŞ 4) , GEORGE MIHAI NIŢULESCU 6) , ŞTEFANIA-FELICIA BĂRBUCEANU 3)

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Design & synthesis of novel oxazolone & triazinone derivatives and their biological evaluation as COX-2 inhibitors

Cited by 24 publications

References 18 publications

The Current Status of O‐Heterocycles: A Synthetic and Medicinal Overview

The Current Status of O‐Heterocycles: A Synthetic and Medicinal Overview

Synthesis, characterization and Cytotoxicity Evaluation of New Compounds from Oxazol-5(4H)-Ones and 1,2,4-Triazin-6(5H)-Ones Classes

New 2-(4-(4-bromophenylsulfonyl)phenyl)-4-arylidene-oxazol-5(4H)-ones: analgesic activity and histopathological assessment

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