Synthesis, Molecular Docking, Analgesic, and Anti-Inflammatory Activities of New 1,2,4-Oxadiazolo-Sulfonamides

Bhargavi, Manan; Shashikala, P.; Sumakanth, Mogili; Challa, Krishna

doi:10.1134/s1070363218040278

Cited by 13 publications

(6 citation statements)

References 20 publications

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“…Research Article (HDSirt2), 55 carbonic anhydrase (CA), 56 histone deacetylase (HDAC), 57 and cyclooxygenase-2 (COX-2). [58][59][60] Moreover, numerous 1,2,4-oxadiazole derivatives have received FDA approval and are now being marketed as pharmaceutical products. 53 Quisqualic acid (Fig.…”

Section: Rsc Medicinal Chemistrymentioning

confidence: 99%

Design, synthesis, and biological evaluation of 1,2,4-oxadiazole-based derivatives as multitarget anti-Alzheimer agents

Ayoup,

Barakat,

Abdel-Hamid

et al. 2024

RSC Med. Chem.

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Section: Rsc Medicinal Chemistrymentioning

confidence: 99%

Design, synthesis, and biological evaluation of 1,2,4-oxadiazole-based derivatives as multitarget anti-Alzheimer agents

Ayoup,

Barakat,

Abdel-Hamid

et al. 2024

RSC Med. Chem.

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“…In addition, 1,2,4-oxadiazole analogues have the advantages of high stability in aqueous solution and resistance to the hydrolysis reaction and are even stable in concentrated sulfuric acid, thus an oxadiazole ring is usually used as bio-isosteres of carbonyl-containing groups (such as esters, amides, and carbamates) in drug discovery and development . Mounting research studies reveal a broad spectrum of biological activities of 1,2,4-oxadiazole derivatives, including the anticancer activity, − antioxidant effect, antibacterial activity, , antiviral activity, anti-inflammatory activity, − and antiparasitic activity, thus attracting growing attention to the role of 1,2,4-oxadiazole heterocyclic analogues in drug discovery …”

Section: Introductionmentioning

confidence: 99%

Target Fishing Reveals a Novel Mechanism of 1,2,4-Oxadiazole Derivatives Targeting Rpn6, a Subunit of 26S Proteasome

Dai

Chen

et al. 2022

J. Med. Chem.

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1,2,4-Oxadiazole derivatives, a class of Nrf2-ARE activators, exert an extensive therapeutic effect on inflammation, cancer, neurodegeneration, and microbial infection. Among these analogues, DDO-7263 is the most potent Nrf2 activator and used as the core structure for bioactive probes to explore the precise mechanism. In this work, we obtained compound 7, a mimic of DDO-7263, and biotin-labeled and fluorescein-based probes, which exhibited homologous biological activities to DDO-7263, including activating Nrf2 and its downstream target genes, anti-oxidative stress, and anti-inflammatory effects. Affinity chromatography and mass analysis techniques revealed Rpn6 as the potential target protein regulating the Nrf2 signaling pathway. In vitro affinity experiments further confirmed that DDO-7263 upregulated Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. These results indicated that Rpn6 is a promising candidate target to activate the Nrf2 pathway for protecting cells and tissues from oxidative, electrophilic, and exogenous microbial stimulation.

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“…Nitrogen- and oxygen-containing heterocyclic compounds have become a hotspot in the field of new pesticide development due to their diversity of molecular structures and their breadth of biological activities [ 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 ]. The 1,2,4-oxadiazole heterocycle, a bioisostere of amides, exhibits certain insecticidal [ 9 , 10 ], antifungal [ 11 , 12 , 13 ], herbicidal [ 14 ], hypotensive [ 15 ] and antitumor activities [ 16 ] in the biological field. In addition, pyrazoleamides exhibit good insecticidal and fungicidal activities [ 17 , 18 , 19 , 20 ], such as tebufenpyrad, penflufen, chlorantraniliprole [ 21 ], penthiopyrad [ 22 ], cyantraniliprole and sedaxane [ 23 ] ( Figure 1 ).…”

Section: Introductionmentioning

confidence: 99%

Structure-Based Bioisosterism Design, Synthesis, Biological Activity and Toxicity of 1,2,4-Oxadiazole Substituted Benzamides Analogues Containing Pyrazole Rings

Shao

Yang

et al. 2022

Molecules

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In order to discover pesticidal lead compounds with high activity and low toxicity, a series of novel benzamides substituted with pyrazole-linked 1,2,4-oxadiazole were designed via bioisosterism. The chemical structures of the target compounds were confirmed via 1H NMR, 13C NMR and HRMS analysis. The preliminary bioassay showed that most compounds exhibited good lethal activities against Mythimna separate, Helicoverpa armigera, Ostrinia nubilalis and Spodoptera frugiperda at 500 mg/L. Particularly in the case of Mythimna separate, compound 14q (70%) exhibited obvious insecticidal activity. In addition, compound 14h demonstrated good fungicidal activity against Pyricularia oryae with an inhibition rate of 77.8%, and compounds 14e, 14k, 14n and 14r also showed certain antifungal activities (55.6–66.7%). The zebrafish toxicity test showed that the LC50 of compound 14h was 14.01 mg/L, which indicated that it may be used as a potential leading compound for further structural optimization.

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Synthesis, Molecular Docking, Analgesic, and Anti-Inflammatory Activities of New 1,2,4-Oxadiazolo-Sulfonamides

Cited by 13 publications

References 20 publications

Design, synthesis, and biological evaluation of 1,2,4-oxadiazole-based derivatives as multitarget anti-Alzheimer agents

Design, synthesis, and biological evaluation of 1,2,4-oxadiazole-based derivatives as multitarget anti-Alzheimer agents

Target Fishing Reveals a Novel Mechanism of 1,2,4-Oxadiazole Derivatives Targeting Rpn6, a Subunit of 26S Proteasome

Structure-Based Bioisosterism Design, Synthesis, Biological Activity and Toxicity of 1,2,4-Oxadiazole Substituted Benzamides Analogues Containing Pyrazole Rings

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