A Review on Oxadiazoles as a Pharmacologically Active Nucleus
Journal of Pharmaceutical Research International · pp. 10–27 · Published 2 Jan 2022
10.9734/jpri/2022/v34i1A35342Abstract
The structure of the oxadiazole skeleton is a biologically and biochemically active nucleus that has a multiple number of biological activities. The oxadiazole structure is a five-membered aromatic ring that has been used in numerous studies and molecules synthesised in laboratories. The principle structure of the Oxadiazole ring with a pair of Pyridine-type nitrogen atoms has been confirmed to be valuable for Oxadiazole analogues for having efficacious protein interactions with a large number of enzyme proteins and receptor proteins present in the organ system of the human body through different types of interactions, like Vander Wall interactions, thereby producing a huge variety of biological activities or pharmacological properties. Due to the variety in the pharmacological activity of Oxadiazole and their derivatives and analogues, they have been termed as one of the important pharmacological aspects to study. Multiple numbers of oxadiazole related synthetic compounds possessing high potent action and therapeutic activity are being widely incorporated for treatment and management of multiple diseases and disorders, giving immeasurable progression and establishment value. Oxadiazole derivatives express a multiple number of pharmacological activities like antimicrobial, anti-inflammatory, analgesic, antifungal, antipyretic, antidepressant, anti-tubercular, anticonvulsant, anticholinesterase, antihypertensive, antidiabetic, antitumor/anticancer, anti-HIV, antioxidant, etc. The history of 1,3,4-Oxadiazole is also very interesting. It shows that it attracted many chemists, researchers, and scientists to explore the Oxadiazole nucleus as a biologically active molecule having promising potency. This review article mainly focuses on the pharmacological profile of 1,3,4-Oxadiazole with various activities and examples (in the form of figures and structures). Expectations are that this article will be like a path showing torch to help and serve as guidance for new innovations/ideas along the progression of research for the evolution of more active/potent and less poisonous/toxic Oxadiazole-based derivatives.
References (51)
- 1 Synthesis and antitumor evaluation of some new 1,3,4-oxadiazole-based heterocycles [DOI]
- 2 1,3,4-Oxadiazoles: An emerging scaffold to target growth factors, enzymes and kinases as anticancer agents [DOI]
- 3 Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles [DOI]
- 4 Synthesis of benzimidazolyl-1,3,4-oxadiazol-2ylthio-N-phenyl (benzothiazolyl) acetamides as antibacterial, antifungal and antituberculosis agents [DOI]
- 5 Synthesis and antioxidant activity of 1,3,4-oxadiazole tagged thieno[2,3-d]pyrimidine derivatives [DOI]
- 6 Synthesis and antimicrobial studies of a new series of 2-{4-[2-(5-ethylpyridin-2-yl)ethoxy]phenyl}-5-substituted-1,3,4-oxadiazoles [DOI]
- 7 Synthesis of benzimidazoles bearing oxadiazole nucleus as anticancer agents [DOI]
- 8 Synthesis, characterization and biological activity of some new 1,3,4-oxadiazole bearing 2-flouro-4-methoxy phenyl moiety [DOI]
- 9 Design, synthesis and biological evaluation of a novel series of 1,3,4-oxadiazole bearing N-methyl-4-(trifluoromethyl)phenyl pyrazole moiety as cytotoxic agents [DOI]
- 10 New indole based hybrid oxadiazole scaffolds with N-substituted acetamides: As potent anti-diabetic agents [DOI]
- 11 Synthesis and evaluation of novel 4-nitropyrrole-based 1,3,4-oxadiazole derivatives as antimicrobial and anti-tubercular agents [DOI]
- 12 N -heterocyclic carbenes (NHC) with 1,2,4-oxadiazole-substituents related to natural products: Synthesis, structure and potential antitumor activity of some corresponding gold(I) and silver(I) complexes [DOI]
- 13 Synthesis, molecular modeling and biological evaluation of 2-aminomethyl-5-(quinolin-2-yl)-1,3,4-oxadiazole-2(3H)-thione quinolone derivatives as novel anticancer agent [DOI]
- 14 Synthesis of novel 1,2,4-oxadiazoles and analogues as potential anticancer agents [DOI]
- 15 Synthesis, characterization, evaluation and molecular dynamics studies of 5, 6–diphenyl–1,2,4–triazin–3(2 H )–one derivatives bearing 5–substituted 1,3,4–oxadiazole as potential anti–inflammatory and analgesic agents [DOI]
- 16 Synthesis and anticancer evaluation of new lipophilic 1,2,4 and 1,3,4-oxadiazoles [DOI]
- 17 Design, synthesis and anticancer activity of new monastrol analogues bearing 1,3,4-oxadiazole moiety [DOI]
- 18 S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents [DOI]
- 19 Synthesis and antioxidant activity of novel Mannich base of 1,3,4-oxadiazole derivatives possessing 1,4-benzodioxan [DOI]
- 20 Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives [DOI]
- 21 Design, synthesis and biological evaluation of 2-(phenoxymethyl)-5-phenyl-1,3,4-oxadiazole derivatives as anti-breast cancer agents [DOI]
- 22 Synthesis, characterization and antibacterial activity of 2-[1-(5-chloro-2-methoxy-phenyl)-5-methyl-1H-pyrazol-4-yl]-5-(substituted-phenyl)-[1,3,4]oxadiazoles [DOI]
- 23 Synthesis, antibacterial evaluation and QSAR studies of 7-[4-(5-aryl-1,3,4-oxadiazole-2-yl)piperazinyl] quinolone derivatives [DOI]
- 24 Synthesis of novel 5-(2,5-bis(2,2,2-trifluoroethoxy)phenyl)-1,3,4-oxadiazole-2-thiol derivatives as potential glucosidase inhibitors [DOI]
- 25 Synthesis, molecular modeling and biological evaluation of 2-(benzylthio)-5-aryloxadiazole derivatives as anti-tumor agents [DOI]
- 26 New lipophilic isoniazid derivatives and their 1,3,4-oxadiazole analogues: Synthesis, antimycobacterial activity and investigation of their mechanism of action [DOI]
- 27 New 1,3,4-Oxadiazole Derivatives of Pyridothiazine-1,1-Dioxide with Anti-Inflammatory Activity [DOI]
- 28 Synthesis and evaluation of some new 1,3,4-oxadiazoles bearing thiophene, thiazole, coumarin, pyridine and pyridazine derivatives as antiviral agents [DOI]
- 29 A solvent free, four-component synthesis and 1,3-dipolar cycloaddition of 4(H)-pyrans with nitrile oxides: Synthesis and discovery of antimycobacterial activity of enantiomerically pure 1,2,4-oxadiazoles [DOI]
- 30 Re-engineering nalidixic acid’s chemical scaffold: A step towards the development of novel anti-tubercular and anti-bacterial leads for resistant pathogens [DOI]
- 31 Synthesis and Antibacterial Evaluation of Novel 1,3,4-Oxadiazole Derivatives Containing Sulfonate/Carboxylate Moiety [DOI]
- 32 Synthesis, characterization and molecular docking studies of some new 1,3,4-oxadiazolines bearing 6-methylpyridine moiety for antimicrobial property [DOI]
- 33 Synthesis of some new 2-(3-methyl-7- substituted-2-oxoquinoxalinyl) -5-(aryl)-1,3,4-oxadiazoles as potential non-steroidal anti-inflammatory and analgesic agents
- 34 Identification and development of 2,5-disubstituted oxadiazole as potential candidate for treatment of XDR and MDR tuberculosis [DOI]
- 35 Novel 3-Acetyl-2,5-disubstituted-1,3,4-oxadiazolines: Synthesis and Biological Activity [DOI]
- 36 Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives [DOI]
- 37 Synthesis of Some 1,3,4‐Oxadiazole Derivatives as Potential Antiinflammatory Agents. [DOI]
- 38 Design, synthesis, and pharmacological evaluation of fluorinated azoles as anti‐tubercular agents [DOI]
- 39 Design and synthesis of 7-diethylaminocoumarin-based 1,3,4-oxadiazole derivatives with anti-acetylcholinesterase activities [DOI]
- 40 Synthesis and characterization of 2, 5-disubstituted-1, 3, 4-oxadiazoles as potential anti-inflammatory agents [DOI]
- 41 Design, Synthesis and QSAR Studies on a Series of 2, 5-Disubstituted- 1,3,4-oxadiazole Derivatives of Diclofenac and Naproxen for Analgesic and Anti-inflammatory Activity [DOI]
- 42 Synthesis and pharmacological activities of some new 5-substituted-2-mercapto-1,3,4-oxadiazoles [DOI]
- 43 Synthesis of Some New Fluorine Containing 1,3,4‐Oxadiazole Derivatives as Potential Antibacterial and Anticancer Agents. [DOI]
- 44 SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME HETEROCYCLES CONTAINING OXADIAZOLE AND PYRAZOLE RING FOR ANTI-BACTERIAL, ANTI-FUNGAL AND ANTI-TUBERCULAR ACTIVITIES [DOI]
- 45 Synthesis and QSAR studies of thiosemicarbazides, 1,2,4-triazoles, 1,3,4- thiadiazoles and 1,3,4-oxadiazoles derivatives as potential antibacterial agents
- 46 Design, synthesis and pharmacological evaluation of 1,3,4-oxadizole derivatives of aryl acetic acid as anti-inflammatory and analgesic agents
- 47 Synthesis and antimicrobial activity of some thiazole and 1,3,4-oxadiazole hybrid heterocycles
- 48 Synthesis and Anticancer Activity of 3, 5-Diaryl 1, 2, 4-Oxadiazole Derivatives
- 49 Synthesis, antimicrobial and antitubercular activity of some novel [3-isonicotinoyl-5-(4-substituted)-2,3-dihydro-1,3,4-oxadiazol-2-yl] and substituted 5-(pyridin-4-yl)-1,3,4-oxadiazole-2-thiol derivatives
- 50 International Journal of Molecular Sciences [DOI]
- 51 INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY [DOI]
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