Synthesis and Biological Activities of Oxadiazole Derivatives: A Review

Vaidya, Ankur; Jain, Shweta; Jain, Priyanka; Jain, Prachi; Tiwari, Nidhi; Jain, Rishabh; Jain, Rashi; Jain, Abhishek Kumar; Agrawal, Ram Kishore

doi:10.2174/1389557516666160211120835

Cited by 70 publications

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“…[ 17 ] These are promising scaffolds of biologically active compounds, isolated from natural products. [ 18 ] Researchers mainly focused on the synthesis of 1,2,4‐oxadiazole derivatives in medicinal chemistry [ 19 ] due to their remarkable biological activities, such as anticancer, [ 20 ] antibiotic, [ 21 ] antifungal, [ 22 ] antioxidant, [ 23 ] anti‐inflammatory, [ 24 ] and anticonvulsant activities. [ 25 ] Recently, several 1,2,4‐oxadiazole derivatives were reported having anticancer activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, cytotoxicity, and molecular docking of substituted 3‐(2‐methylbenzofuran‐3‐yl)‐5‐(phenoxymethyl)‐1,2,4‐oxadiazoles

Mokenapelli

Thalari

Vadiyaala

et al. 2020

Archiv der Pharmazie

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A series of new benzofuran/oxadiazole hybrids (8a-n) was synthesized from 2H-chromene-3-carbonitriles (3a-c) through the multistep synthetic methodology, and these hybrids are known to exhibit anticancer activities. All the compounds were evaluated for their in vitro cytotoxicity against the HCT116 and MIA PaCa2 cell lines. Compounds 6a (IC 50 : 9.71 ± 1.9 μM), 6b (IC 50 : 7.48 ± 0.6 μM), and 6c (IC 50 : 3.27 ± 1.1 μM) displayed a significant cytotoxic activity, whereas compounds 8d and 8e exhibited good activity against both cell lines. The depletion of glycogen synthase kinase-3β (GSK3β) induces apoptosis through the inhibition of basal NF-κB activity in HCT116 colon cancer cells and MIA PaCa2 pancreatic cancer cells. Molecular docking of compounds 6a, 6b, 6c, 8d, and 8e with GSK3β demonstrated the best binding affinity, correlating with the biological activity assay. Furthermore, the structure-activity relationship of these novel compounds reveals promising features for their use in anticancer therapy. K E Y W O R D S 1,2,4-oxadiazole, benzofuran, cytotoxicity, docking studies, glycogen synthase kinase-3β 2 of 12 | MOKENAPELLI ET AL.

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Section: Introductionmentioning

confidence: 99%

Synthesis, cytotoxicity, and molecular docking of substituted 3‐(2‐methylbenzofuran‐3‐yl)‐5‐(phenoxymethyl)‐1,2,4‐oxadiazoles

Mokenapelli

Thalari

Vadiyaala

et al. 2020

Archiv der Pharmazie

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“…54 There are several reviews in the literature of 1,2,4-and 1,3,4-oxadiazoles focusing on their synthesis and applications. 55 In spite of that, the present work is the first review highlighting the importance of these heterocycles specifically in the development of new drugs with antiparasitic properties.…”

Section: Synthesis Of 134-oxadiazolesmentioning

confidence: 94%

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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“…Besides, 1,3,4‐oxadiazoles presence worthy bioisosteres of amides and esters may work together with the receptors by making proton bonding and possibly raise the biotic profile significantly . Several biologically active oxadizoles have been reported previously . Biotic capacities of oxadiazoles were also reported in the literature as anticancer , antiproliferative , anti‐HIV , anti‐inflammatory , antitubercular , antimicrobial , anticonvulsant , antimalarial , antihepatitis B viral activities , and many more.…”

Section: Introductionmentioning

confidence: 98%

Multicomponent One‐pot Synthesis of Oxadiazole Included Pyranopyrazoles as Promising Antioxidant Agents

Reddy

Chen

Subbaiah

et al. 2019

Journal of Heterocyclic Chem

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Oxadiazole‐fused combinations are of great concern for the novelty of effective therapeutic agents. In this context, a series of oxadiazole included pyranopyrazoles were prepared under eco‐friendly synthetic way by using montmorillonite k10 as a catalyst. All the final outcomes were formed with good yields. Further, compounds screened for their antioxidant assay. Most of the compounds revealed promising activity. Among all outcomes, electron rich‐substituted compounds at para position demonstrated higher antioxidant activity than their corresponding ortho‐substituted compounds. All belongings concluded that this eco‐friendly path is preferable to prepare therapeutic compounds. Further, biotic results established that all these biologically active compounds fit for supplementary to develop exogenous antioxidant drugs.

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Synthesis and Biological Activities of Oxadiazole Derivatives: A Review

Cited by 70 publications

References 0 publications

Synthesis, cytotoxicity, and molecular docking of substituted 3‐(2‐methylbenzofuran‐3‐yl)‐5‐(phenoxymethyl)‐1,2,4‐oxadiazoles

Synthesis, cytotoxicity, and molecular docking of substituted 3‐(2‐methylbenzofuran‐3‐yl)‐5‐(phenoxymethyl)‐1,2,4‐oxadiazoles

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

Multicomponent One‐pot Synthesis of Oxadiazole Included Pyranopyrazoles as Promising Antioxidant Agents

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