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Journal articles on the topic 'Oxadiazole derivative'

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Published: 3 June 2025

Last updated: 1 August 2025

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1

Rachel, Mathew* V. .S. Anjana Ayoona Najeeb Fathima Shereen S. Nikhila Anna Anil Saranya B. Sarin Santhosh. "COMMENCEMENT SCRUTINY OF 1,3,4-OXADIAZOLE; ITS VISCERAL ACTIVITIES." International Journal in Pharmaceutical Sciences 2, no. 5 (2024): 1265–74. https://doi.org/10.5281/zenodo.11264100.

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Oxadiazoles are a class of heterocyclic aromatic chemical compound of the azole family.1,3,4-oxadiazole is a nitrogen and oxygen containing heterocyclic derivative in which nitrogen in 3rd and 4th positions and oxygen in 1st position with chemical formula, C2 H2N2O and molecular weight 70.051g.mol-1. 1,3,4- oxadiazole is also known asOxdiazole,1-Oxa-3,4diazacyclopentadiene. 1,3,4- oxadiazole and its derivatives were used by several chemists for therapeutic conditions because it posses many pharmacological activities. 1,3,4- oxadiazole and its derivatives have great significance in medicinal ch

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2

Amer, Hamada, Omar Ali, Akram Salama, Marwa gendy та Omima Houssin. "Synthesis of some new 1,3,4-oxadiazole derivatives bearing sugars and α-aminophosphonate derived from 4-nitrophenol as anticancer agents". National Journal of Physiology, Pharmacy and Pharmacology 2, № 1 (2018): 1275. https://doi.org/10.5455/njppp.2018.8.0416408052018-1.

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Background: 1,3,4-oxadiazoles square measure a very important category of heterocyclic compounds with a broad variety of biological activities such as medicament, analgesic, ulcerogenicity, apoptosis inducer, anti-mycobacterial, antifungal, antitumor, P-glycoprotein Inhibitors, pesticides, 4-hydroxylase inhibitors, and antiepileptic drug activity. Aims and Objectives: The present study is undertaken to study the evaluation of new 1,3,4-oxadiazole derivatives bearing sugars and α-aminophosphonate derived from 4-nitrophenol as anticancer agents. Materials and Methods: A sequence of acyclic nucle

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3

Santhanalakshmi K., Neelakandeswari N., Jacquline Rosy P., and Margandan K. "An In Vitro Evaluation of Anti-Inflammatory Activity of Newly Synthesized 1,3,4 Oxadiazole Derivatives." International Journal of Zoological Investigations 08, no. 02 (2022): 755–64. http://dx.doi.org/10.33745/ijzi.2022.v08i02.091.

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In the area of heterocyclic chemistry, oxadiazole has made major contributions. An enormous number of oxadiazoles have been synthesized and exposed to biological screening; the screening results improved their status due to its potential activities and their efficacy in diverse fields of daily life. Due to its wide range of pharmacological and therapeutic effects, the 1,3,4-oxadiazole moiety is the most important oxadiazole. In this study, we discuss a new family of 2,5-disubstituted 1,3,4-oxadiazole compounds' anti-inflammatory characteristics (4a-4h).The antiinflammatory efficacy of the oxad

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4

Ho, Vien Q. T., Mark K. Rong, Eva Habjan, et al. "Dysregulation of Mycobacterium marinum ESX-5 Secretion by Novel 1,2,4-oxadiazoles." Biomolecules 13, no. 2 (2023): 211. http://dx.doi.org/10.3390/biom13020211.

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The ESX-5 secretion system is essential for the viability and virulence of slow-growing pathogenic mycobacterial species. In this study, we identified a 1,2,4-oxadiazole derivative as a putative effector of the ESX-5 secretion system. We confirmed that this 1,2,4-oxadiazole and several newly synthesized derivatives inhibited the ESX-5-dependent secretion of active lipase LipY by Mycobacterium marinum (M. marinum). Despite reduced lipase activity, we did not observe a defect in LipY secretion itself. Moreover, we found that several other ESX-5 substrates, especially the high molecular-weight PE

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5

Stepanova, Elena V., and Andrei I. Stepanov. "UNUSUAL WAY OF REACTION OF 3-AMINO-4-(5-CHLOROMETHYL-1,2,4-OXADIAZOLE-3-YL)-FURAZAN WITH HYDRAZINE." IZVESTIYA VYSSHIKH UCHEBNYKH ZAVEDENIY KHIMIYA KHIMICHESKAYA TEKHNOLOGIYA 60, no. 4 (2017): 26. http://dx.doi.org/10.6060/tcct.2017604.5522.

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The results of our study of the pathways of selective reactivity of 3-amino-4-(5-chloromethyl-1,2,4-oxadiazole-3-yl)furazan versus 5-unsubstituted or 5-methyl and 5-trifluoromethyl substituted 4-(5R-1,2,4-oxadiazole-3-yl)furazans (R = H, Me, CF3) towards the action of hydrazine are discussed. If the reductive opening of 1,2,4-oxadiazole ring in unsubstituted at the С-5 atom (1,2,4-oxadiazol-3-yl)furazan derivatives under the treatment with hydrazine can be used as a method for the preparation of a range of amidrazones of 4-R-furazan-3-carboxylic acid. 3-amino-4-(5-trifluoromethyl-1,2,4-oxadiaz

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6

Qazi, Adil Iqbal, Bashir Ahmad, Muhammad Umar Khayam Sahibzada, et al. "Evaluation of Antidiabetic Activity of Oxadiazole Derivative in Rats." Evidence-Based Complementary and Alternative Medicine 2023 (April 25, 2023): 1–15. http://dx.doi.org/10.1155/2023/1141554.

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The oxadiazole ring has long been used for the treatment of several diseases. This study aimed to analyze the antihyperglycemic and antioxidant roles of the 1,3,4-oxadiazole derivative with its toxicity. Diabetes was induced through intraperitoneal administration of alloxan monohydrate at 150 mg/kg in rats. Glimepiride and acarbose were used as standards. Rats were divided into groups of normal control, disease control, standard, and diabetic rats (treated with 5, 10, and 15 mg/kg of 1,3,4-oxadiazole derivative). After 14 days of oral administration of 1,3,4-oxadiazole derivatives (5, 10, and

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7

Irfan, Ali, Shah Faisal, Ameer Fawad Zahoor, et al. "In Silico Development of Novel Benzofuran-1,3,4-Oxadiazoles as Lead Inhibitors of M. tuberculosis Polyketide Synthase 13." Pharmaceuticals 16, no. 6 (2023): 829. http://dx.doi.org/10.3390/ph16060829.

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Benzofuran and 1,3,4-oxadiazole are privileged and versatile heterocyclic pharmacophores which display a broad spectrum of biological and pharmacological therapeutic potential against a wide variety of diseases. This article reports in silico CADD (computer-aided drug design) and molecular hybridization approaches for the evaluation of the chemotherapeutic efficacy of 16 S-linked N-phenyl acetamide moiety containing benzofuran-1,3,4-oxadiazole scaffolds BF1–BF16. This virtual screening was carried out to discover and assess the chemotherapeutic efficacy of BF1–BF16 structural motifs as Mycobac

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8

Ramazani, Ali, Yavar Ahmadi, and Fatemeh Zeinali Nasrabadi. "Four-component Synthesis of 1,3,4-Oxadiazole Derivatives from (N-Isocyanimino)triphenylphosphorane, (E)-Cinnamic Acids, Acetaldehyde and Secondary Amines." Zeitschrift für Naturforschung B 66, no. 2 (2011): 184–90. http://dx.doi.org/10.1515/znb-2011-0211.

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The 1 : 1 iminium intermediate, generated by the addition of a secondary amine to acetaldehyde is trapped by the (N-isocyanimino)triphenylphosphorane in the presence of an (E)-cinnamic acid derivative, leading to the formation of the corresponding iminophosphorane intermediate. Disubstituted 1,3,4-oxadiazole derivatives are formed via intramolecular aza-Wittig reaction of the iminophosphorane intermediates. The reactions were completed under neutral conditions at room temperature, and the corresponding disubstituted 1,3,4-oxadiazole derivatives were produced in excellent yields.

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Das, Rina, and Dinesh Kumar Mehta. "Evaluation and Docking Study of Pyrazine Containing 1, 3, 4-Oxadiazoles Clubbed with Substituted Azetidin-2-one: A New Class of Potential Antimicrobial and Antitubercular." Drug Research 71, no. 01 (2020): 26–35. http://dx.doi.org/10.1055/a-1252-2378.

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Abstract Background Tuberculosis (TB) caused by Mycobacterium tuberculosis is one of the main killers of people all over the world. The major hurdles with existing therapy are the lengthy regimen and appearance of multi drug resistant (MDR) and extensively drug resistant (XDR) strains of M.tuberculosis. Aims The present work was aimed to synthesize and determine antitubercular and antimicrobial potential of some novel 3-chloro-4-aryl-1-[4-(5-pyrazin-2-yl[1,3,4]oxadiazole-2-ylmethoxy)-phenyl]-azetidin-2-one derivatives 7(a-h) from pyrazinoic acid as precursor, which is a well-established antitu

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Ekram Abdullah Basheer, Kalid Matny Al-jaanaby, and Feras Shauki Al-joboury. "Synthesis a Number of Heterocyclic Compounds Derived From Levofloxacin." Tikrit Journal of Pure Science 20, no. 5 (2023): 84–95. http://dx.doi.org/10.25130/tjps.v20i5.1244.

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In this paper, the preparation a number of heterocyclic compounds five membered rings like oxadiazole, imidazolidine, thiozolidine, tetrazole, azetidine 2-on. Hydrazide (1) was synthesized from the reaction of levofloxacin with hydrazine hydrate. Hydrazone compounds (2-9) were synthesized from the reaction (1) with a number of aldehydes, and 3-acetyl-1,3,4-oxadiazol (10-17) was prepared from the reaction of hydrazones (2-9) with acetic anhydride, 5-oxo-2-aryl imadazoldine derivative (18-25) were prepared from the reaction of hydrazone derivatives (2-9) with glycine, while the reaction of hydra

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11

Yadav, Mange, Shrikant Shirude, Devendra Puntambekar, et al. "Studies in 3,4-diaryl-1,2,5-oxadiazoles and their N-oxides: Search for better COX-2 inhibitors." Acta Pharmaceutica 57, no. 1 (2007): 13–30. http://dx.doi.org/10.2478/v10007-007-0002-z.

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Studies in 3,4-diaryl-1,2,5-oxadiazoles and theirN-oxides: Search for better COX-2 inhibitorsA series of 3,4-diaryl-1,2,5-oxadiazoles and 3,4-diaryl-1,2,5-oxadiazoleN-oxides were prepared and evaluated for COX-2 and COX-1 binding affinityin vitroand for anti-inflammatory activity by the rat paw edema method.p-Methoxy (p-OMe) substituted compounds 9, 21, 34, 41, 42 showed COX-2 enzyme inhibition higher than that showed by compounds with other substituents. 3,4-Di(4-methoxyphenyl)-1,2,5-oxadiazoleN-oxide (42) showed COX-2 enzyme inhibition of 54% at 22 μmol L-1and COX-1 enzyme inhibition of 44%

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G., Nagaraju 1. *. Dr. Anil Kumar 2. "SYNTHESIS, CHARACTERISATION AND BIOLOGICAL ACTIVITIES OF OXADIAZOLE DERIVATIVE." Journal of Pharma Research 7, no. 6 (2018): 96–98. https://doi.org/10.5281/zenodo.1291605.

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<strong><em>ABSTRACT</em></strong> <strong><em>I</em></strong><em>satin chemically known as 1H-indole-2,3-dione. It is a unique molecule possessing both amide and keto carbonyl groups. Isatin and its derivatives having several pharmacological actions. In the present study some Isatins derivatives have been synthesized.  The chemical structures of the synthesized compounds were confirmed by using spectral and elemental analysis methods and developed some pharmacological evaluations.</em> <strong><em>KEY WORDS:</em></strong><em> Isatins, Pharmacological actions,<strong> </strong>Oxadiazole

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13

Journal, Baghdad Science. "Synthesis and Characterization of 1,3,4-Oxadiazoles Derived From 9-Fluorenone." Baghdad Science Journal 10, no. 2 (2013): 449–61. http://dx.doi.org/10.21123/bsj.10.2.449-461.

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In the present work, 9-fluorenone-2-carboxylic acid methyl ester (1) was prepared from 9-fluorenone-2-carboxylic acid and then converted into the acid hydrazide (2). Compound (2), is the key intermediate for the synthesis of several series of new compounds such as substituted 1,3,4-oxadiazole derivatives (3-6) were synthesized from the condensation of different substituted benzoic acids with compound (2) using POCl3 as condensing agent. Treatment of compound (2) with formic acid gave the N-formyl hydrazide (7), which upon refluxing with phosphorous pentoxide in benzene yielded the correspondin

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14

Dawood, Rafid Saad. "Synthesis and Characterization of 1,3,4-Oxadiazoles Derived From 9-Fluorenone." Baghdad Science Journal 10, no. 2 (2013): 449–61. http://dx.doi.org/10.21123/bsj.2013.10.2.449-461.

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In the present work, 9-fluorenone-2-carboxylic acid methyl ester (1) was prepared from 9-fluorenone-2-carboxylic acid and then converted into the acid hydrazide (2). Compound (2), is the key intermediate for the synthesis of several series of new compounds such as substituted 1,3,4-oxadiazole derivatives (3-6) were synthesized from the condensation of different substituted benzoic acids with compound (2) using POCl3 as condensing agent. Treatment of compound (2) with formic acid gave the N-formyl hydrazide (7), which upon refluxing with phosphorous pentoxide in benzene yielded the correspondin

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15

Kumar, Vikash, Ravindra Kumar, Nagendra Kumar, and Sumit Kumar. "Solvation Dynamics of Oxadiazoles as Potential Candidate for Drug Preparation." Asian Journal of Chemistry 35, no. 4 (2023): 991–98. http://dx.doi.org/10.14233/ajchem.2023.27594.

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Oral ingestion is one of the popularly employed procedures for the drug delivery as the administration of drugs is easy compared to the other alternatives such as injection. Therefore, the drug preparation is affected by dissolution rate, metabolism as per system requirements, drug permeability as well as solubility of the drug. The current study focused on the solvation dynamics of oxadiazole derivatives to attain its candidature against drug preparation. Different derivatives are extensively explored using ab initio molecular dynamics and quantum chemical calculation tools. The molecular dyn

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16

Cellupica, Edoardo, Aureliano Gaiassi, Ilaria Rocchio, et al. "Mechanistic and Structural Insights on Difluoromethyl-1,3,4-Oxadiazole Inhibitors of HDAC6." International Journal of Molecular Sciences 25, no. 11 (2024): 5885. http://dx.doi.org/10.3390/ijms25115885.

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Histone deacetylase 6 (HDAC6) is increasingly recognized for its potential in targeted disease therapy. This study delves into the mechanistic and structural nuances of HDAC6 inhibition by difluoromethyl-1,3,4-oxadiazole (DFMO) derivatives, a class of non-hydroxamic inhibitors with remarkable selectivity and potency. Employing a combination of nuclear magnetic resonance (NMR) spectroscopy and liquid chromatography-mass spectrometry (LC-MS) kinetic experiments, comprehensive enzymatic characterizations, and X-ray crystallography, we dissect the intricate details of the DFMO-HDAC6 interaction dy

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17

Bąchor, Urszula, Ewa Drozd-Szczygieł, Remigiusz Bąchor, Lucjan Jerzykiewicz, Robert Wieczorek, and Marcin Mączyński. "New water-soluble isoxazole-linked 1,3,4-oxadiazole derivative with delocalized positive charge." RSC Advances 11, no. 47 (2021): 29668–74. http://dx.doi.org/10.1039/d1ra05116d.

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18

Patel, Navin, Sabir Pathan, and Hetal I. Soni. "3,4-Dihydropyrimidin-2(1H)-One Analogues: Microwave irradiated Synthesis with Antimicrobial and Antituberculosis Study." Current Microwave Chemistry 6, no. 1 (2019): 61–70. http://dx.doi.org/10.2174/2213335606666190724093305.

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Background: For rapid and sustainable synthesis, microwave irradiation method is serviceable. This present study deals with the preparation of oxadiazole and pyridine bearing 1,2,3,4- tetrahydro pyrimidine derivatives by microwave irradiation. Objective: The present study aims to carry out rapid synthesis of chloro-acetamides of oxadiazoles of Biginelli product and amino cyano derivative of pyridine by microwave-assisted heating. Our efforts are focused on the introduction of chemical diversity in the molecular framework in order to synthesize pharmacologically interesting compounds. Methods::

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19

Naji, Amel Mohson, Ahmed Mutanabbi Abdula, Olfat A. Nief, and Ebtihal K. Abdullah. "Synthesis, Characterization, Antimicrobial and Molecular Docking Study of Benzooxadiazole Derivatives." Chemistry & Chemical Technology 16, no. 1 (2022): 25–33. http://dx.doi.org/10.23939/chcht16.01.025.

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In this study, a series of new1,2,5-oxadiazole compounds derived from 4-chloro-7-nitro-benzo 1,2,5-oxadiazole was synthesized using different organic procedures. The resulting derivatives were chemically characterized and their structures were confirmed by FT-IR and NMR analysis. All the compounds were also evaluated for their antibacterial and antifungal activity against four types of pathogenic bacteria: S.aureus, S.epidermidis (as gram-negative bacteria), E.coli, Klebsiella spp. (as gram-positive bacteria) and the fungus Candida albicans using the agar well diffusion method. The synthesized

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A. Abdulqader, Kany, Ahmed W. Naser, Muthanna S. Farhan та Sabah J. Salih. "Synthesis, Characterization and Cytotoxic Activity of some new 1,2,3-Triazole, Oxadiazole and Aza- β-lactam Derivatives". Oriental Journal of Chemistry 34, № 5 (2018): 2350–60. http://dx.doi.org/10.13005/ojc/340516.

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A series of 1,2,3-triazole, oxadiazole and aza-β-lactam derivatives were synthesized through consecutive reaction began from o-(N-propargyl) sulfonamido benzoic acid (1a). The reaction of (1a) with absolute ethanol in the presence of concentrated H2SO4 resulted in the formation of ester derivative (2a). The product of the previous reaction was reacted with 80% hydrazine hydrate to prepare benzohydrazide derivative (3a). 1,3,4-oxadiazole compound (4a) was obtained by condensation of compound (3a) with CS2 in presence KOH . Compound (3a) react with Phenyl isocyanates to give Carboxamide derivati

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Patidar, Mohini, Raghvendra Dubey, and Nitin Deshmukh. "Exploring 1,3,4-oxadiazole derivatives for hepatocellular carcinoma: synthesis, and bioactivity evaluation." Journal of Applied Pharmaceutical Research 13, no. 2 (2025): 127–38. https://doi.org/10.69857/joapr.v13i2.1008.

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Background: Cancer is a leading cause of death globally, with existing treatments often limited by resistance and toxicity. This necessitates the development of new, more effective anticancer therapies. Methodology: This study used In-silico modeling with tools like Pre-ADMET and Molinspiration to evaluate the physicochemical, pharmacokinetic, and pharmacodynamic properties of substituted 1,3,4-Oxadiazole derivatives. Results and discussion: Computational studies of 1,3,4-Oxadiazole analogues showed promising drug-like properties and bioavailability. To test the inhibitory efficacy against the

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El-Essawy, Farag A., Wael A. El-Sayed, Sherif A. El-Kafrawy, Asmaa S. Morshedy, and Adel-H. Abdel-Rahman. "Anti-Hepatitis B Virus Activity of New 1,2,4-Triazol-2-yl- and 1,3,4-Oxadiazol-2-yl-2-pyridinone Derivatives." Zeitschrift für Naturforschung C 63, no. 9-10 (2008): 667–74. http://dx.doi.org/10.1515/znc-2008-9-1010.

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A number of 1,3,4-oxadiazole, 3 - 9, and 1,2,4-triazole derivatives, 13 - 15, were synthesized starting form the acid hydrazide 1. The 1,3,4-thiadiazole derivative 12 was prepared from the substituted phenylthiosemicarbazide derivative 11 by treatment with sulfuric acid. The aryl hydrazone derivatives 10a - c were synthesized by reaction of the hydrazide 1 with the corresponding ketones. The thioalkyl derivatives 16a - e were prepared by akylation of the thiol derivatives 3 and 13 with different alkylating agents. The newly synthesized compounds were tested for their anti-HBV activity and some

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23

Jalhan, Sunny. "Review Article: Various Biological Activities of Coumarin and Oxadiazole Derivatives." Asian Journal of Pharmaceutical and Clinical Research 10, no. 7 (2017): 38. http://dx.doi.org/10.22159/ajpcr.2017.v10i7.18461.

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In this review article data is collected regarding the various derivatives of coumarin and oxadiazole as both these have wide range of biological activities and they can be further modified to synthesize more effective and potent drugs. Coumarin class of organic compounds consists of 1,2-benzopyrone ring system as a basic parent scaffold. These benzopyrones are subdivided into alpha-benzopyrones and gamma benzopyrones; with coumarin class of compounds belonging to alpha-benzopyrones. Since the last few years, coumarins were synthesized in many of their derivative forms. Their pharmacological,

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24

Elhady, Heba A., and Hossa F. Al-Shareef. "Synthesis, Characterization, Anti-proliferative Evaluation, and DNA Flow Cytometry Analysis of Some 2-Thiohydantoin Derivatives." Mini-Reviews in Medicinal Chemistry 20, no. 18 (2020): 1929–41. http://dx.doi.org/10.2174/1389557520666200611093510.

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Background and Objective: Due to the well-documented anti-proliferative activity of 2-thiohydantoin incorporated with pyrazole, oxadiazole, quinazoline, urea, β-naphthyl carbamate and Schiff bases, they are noteworthy in pharmaceutical chemistry. Methods: An efficient approach for the synthesis of a novel series of 2-thiohydantoin derivatives incorporated with pyrazole and oxadiazole has proceeded via the reaction of the acyl hydrazide with chalcones and/or triethyl orthoformate. Schiff bases were synthesized by the reaction of the acyl hydrazide with different aromatic aldehydes. Moreover, Cu

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Wang, X., W. Wang, H. X. Liu, M. Y. Tan, and M. Li. "A Derivative of 1,3,4-Oxadiazole." Acta Crystallographica Section C Crystal Structure Communications 51, no. 8 (1995): 1585–87. http://dx.doi.org/10.1107/s010827019400510x.

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Ghoorbannejad, Saeed, Dilmaghani Akbari, and Abbas Nikoo. "Synthesis and assessment of the cytotoxic effect of some of 1,4-dihydropyridine derivatives which contain azole moiety." Journal of the Serbian Chemical Society, no. 00 (2021): 64. http://dx.doi.org/10.2298/jsc200818064g.

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A number of 1,4-dihydropyridine derivatives (9a-d, 10a-d, and 11a-d) were designed and synthesized by the reaction of 1,3,4-oxadiazole-5-thiones and 1,2,4-triazole-5-thiones to 2,6-dibromomethyl-3,5-diethoxycarbonyl-4-(3-ni-trophenyl)-1,4-dihydropyridine. The synthesized compounds were characterrized using FT-IR, 1H-NMR, 13C-NMR spectral data, ESI-MS, and elemental analysis. The cytotoxicity of the synthesized compounds was evaluated in human breast cancer (MCF-7) cells based on the results of MTT assay. The results indicated that compound Diethyl 4-(3-nitrophenyl)-2,6-bis[((5-(3-nitrophenyl)-

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SarveAhrabi, Yasin, Nakisa Zarrabi Ahrabi, and Ali Souldozi. "Synthesis and Antimicrobial Evaluation of New Series of 1,3,4-Oxadiazole Containing Cinnamic Acid Derivatives." Avicenna Journal of Clinical Microbiology and Infection 8, no. 1 (2021): 11–16. http://dx.doi.org/10.34172/ajcmi.2021.03.

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Background: New drugs must be designed and synthesized for combating resistant pathogens. In this study, antibacterial and antifungal activities of 4 new derivatives of 1,3,4-oxadiazole were assessed against 8 bacterial and 2 fungal pathogens. Methods: To this end, the cinnamic acid derivatives were dissolved in acetonitrile solvent and N-iso-ciano-imino-triphenyl-phosphorane was added to the above-mentioned solution, followed by applying Petroleum ether and Ethyl acetate as solvent and base. Then, antimicrobial susceptibility tests were used to determine inhibition zone diameter, minimum inhi

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Panchal, Ishan I., Roshani Rajput, and Ashish D. Patel. "Design, Synthesis and Pharmacological Evalution of 1,3,4-Oxadiazole Derivatives as Collapsin Response Mediator Protein 1 (CRMP 1) Inhibitors." Current Drug Discovery Technologies 17, no. 1 (2020): 57–67. http://dx.doi.org/10.2174/1570163815666181106090708.

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Objective: The series of 2-(4-Phenylamino)-N-(5-((4-nitrophenoxy)methyl) -1,3,4-oxadiazol- 2-yl)aceta-mide (5a-5e) and substituted N-(5-(Phenoxymethyl)-1,3,4-oxadiazol-2-yl)-2- (phenylamino)acetamide (5f-5i) was designed, synthesized and investigated for Collapsin Response Mediator Protein 1 (CRMP 1) inhibitors as small lung cancer. Design: Design of compounds was determined by literature review and molecular docking studies in iGEMDOCK 2.0. Materials and Methods: Novel 1, 3, 4 Oxadiazole derivatives were synthesized and characterized by melting point, TLC, IR Spectroscopy, Mass spectroscopy a

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Ngô Thị Châu. "Preparation of benzofuran-2-carbohydrazide and its utilization for benzofuran-bearing 1,2,4-triazole and 1,3,4-oxadiazole synthesis." Journal of Science and Technology 6, no. 1 (2024): 8. http://dx.doi.org/10.55401/51907v37.

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Benzofuran, triazole and oxadiazole spontaneously occur in natural compounds with highly desired bioactivities, such as antibacterial, antifungal, antiviral and anticancer. These cyclic scaffolds happen in a variety of commercial medicines as well as developed drugs in late-stage clinical trials (eg. amiodarone, ramelteon, zibotentan, and ataluren). Benzofuran-bearing triazole and oxadiazole can be synthesized by click reaction, requiring an alkynyl group. The formation of the alkynyl group can be achieved by treating the precursor with sodium azide, a poisonous chemical that needs safe condit

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Ngo, Chau Thi. "Preparation of benzofuran-2-carbohydrazide and its utilization for benzofuran-bearing 1,2,4-triazole and 1,3,4-oxadiazole synthesis." Journal of Science and Technology 6, no. 1 (2023): 8. http://dx.doi.org/10.55401/jst.v6i1.1672.

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Benzofuran, triazole and oxadiazole spontaneously occur in natural compounds with highly desired bioactivities, such as antibacterial, antifungal, antiviral and anticancer. These cyclic scaffolds happen in a variety of commercial medicines as well as developed drugs in late-stage clinical trials (eg. amiodarone, ramelteon, zibotentan, and ataluren). Benzofuran-bearing triazole and oxadiazole can be synthesized by click reaction, requiring an alkynyl group. The formation of the alkynyl group can be achieved by treating the precursor with sodium azide, a poisonous chemical that needs safe condit

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31

Dutra, Luiz Antônio, Letícia de Almeida, Thais G. Passalacqua, et al. "Leishmanicidal Activities of Novel Synthetic Furoxan and Benzofuroxan Derivatives." Antimicrobial Agents and Chemotherapy 58, no. 8 (2014): 4837–47. http://dx.doi.org/10.1128/aac.00052-14.

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ABSTRACTA novel series of furoxan (1,2,5-oxadiazole 2-oxide) (compounds 3, 4a and -b, 13a and -b, and 14a to -f) and benzofuroxan (benzo[c][1,2,5]oxadiazole 1-oxide) (compounds 7 and 8a to -c) derivatives were synthesized, characterized, and evaluated forin vitroactivity against promastigote and intracellular amastigote forms ofLeishmania amazonensis. The furoxan derivatives exhibited the ability to generate nitric oxide at different levels (7.8% to 27.4%). The benzofuroxan derivative 8a was able to increase nitrite production in medium supernatant from murine macrophages infected withL. amazo

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32

Alotaibi, Mshari A., Farag A. El Essawy, and Nader M. Boshta. "Preparation of New Oxadiazole Acyclic Nucleoside and Thioglycoside Analogs Containing Chromene Moiety with Antimicrobial Evaluation." Revista de Chimie 68, no. 10 (2017): 2228–33. http://dx.doi.org/10.37358/rc.17.10.5861.

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New sugar hydrazones linked to chroman ring system and their derived oxadiazole acyclic nucleoside analogs were synthesized from the substituted ethyl ester oxime derivative. The 2-sustituted 1,3,4-oxadiazole-5-thione prepared from acid hydrazide was glycosylated to afford the corresponding thioglycosides, not the N-linked glycosides. The novel compounds were evaluated for their antimicrobial activity and showed different degrees of activities.

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33

Kurfürst, Antonín, Pavel Lhoták, Petr Nádeník, Františka Raclová-Pavlíková, and Josef Kuthan. "2-(Biphenyl-4-yl)-5-phenyl-1,3,4-oxadiazole (PBD): Electrophilic 4’-substitution and following transformations." Collection of Czechoslovak Chemical Communications 56, no. 7 (1991): 1495–504. http://dx.doi.org/10.1135/cccc19911495.

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PBD was converted into 4’-substituted derivatives I-XII using usual electrophilic reagents. The decomposition of PBD, 4’-acetyl derivative I and 4’-nitro derivative VI with hydroiodic acid gave 4’-substituted 4-biphenylcarboxylic acids XIIIa-XIIIc and benzoic acid, respectively. The regioselectivity of the reaction was also proved by means of high resolution NMR spectroscopy.

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34

Et al., Khammas. "Synthesis, Cytotoxicity, Xanthine Oxidase Inhibition, Antioxidant of New Pyrazolo{3,4 d}Pyrimidine Derivatives." Baghdad Science Journal 16, no. 4(Suppl.) (2019): 1003. http://dx.doi.org/10.21123/bsj.2019.16.4(suppl.).1003.

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Allopurinol derivative were prepared by reacting the (1-chloroacetyl)-2-Hydropyrazolo{3,4-d}pyrimidine-4-oneiwith 5- methoxy- 2-aminoibenzothiazoleiunder certain conditions to obtain new compound ( N- (2-aminoacetyl (5-methoxy) benzothiazole -2yl) (A4), Reaction of 5-(P-dimethyl amine benzene)-2-amino-1,3,4- oxadiazole in the presence of potassium carbonate anhydrous to yield new compound (N-(2- aminoacetyl-5-(P-dimethyl amine benzene )-1,3,4-oxadiazoles-2-yl)(A30) and Azo compound (N-(5-(Azo-2-hydroxy-5-amino benzene)-1,3-Diazol-2yl)Allopurinol(A46). The structure of prepared compounds were c

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35

Buommino, Elisabetta, Simona De Marino, Martina Sciarretta, Marialuisa Piccolo, Carmen Festa, and Maria Valeria D’Auria. "Synergism of a Novel 1,2,4-oxadiazole-containing Derivative with Oxacillin against Methicillin-Resistant Staphylococcus aureus." Antibiotics 10, no. 10 (2021): 1258. http://dx.doi.org/10.3390/antibiotics10101258.

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Staphylococcusaureus is an important opportunistic pathogen that causes many infections in humans and animals. The inappropriate use of antibiotics has favored the diffusion of methicillin-resistant S. aureus (MRSA), nullifying the efforts undertaken in the discovery of antimicrobial agents. Oxadiazole heterocycles represent privileged scaffolds for the development of new drugs because of their unique bioisosteric properties, easy synthesis, and therapeutic potential. A vast number of oxadiazole-containing derivatives have been discovered as potent antibacterial agents against multidrug-resist

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36

Bordei Telehoiu, Alexandra T., Diana C. Nuță, Miron T. Căproiu, et al. "Design, Synthesis and In Vitro Characterization of Novel Antimicrobial Agents Based on 6-Chloro-9H-carbazol Derivatives and 1,3,4-Oxadiazole Scaffolds." Molecules 25, no. 2 (2020): 266. http://dx.doi.org/10.3390/molecules25020266.

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In this paper, we aimed to exploit and combine in the same molecule the carbazole and the 1,3,4-oxadiazole pharmacophores, to obtain novel carprofen derivatives, by using two synthesis pathways. For the first route, the following steps have been followed: (i) (RS)-2-(6-chloro-9H-carbazol-2-yl)propanonic acid (carprofen) treatment with methanol, yielding methyl (RS)-2-(6-chloro-9H-carbazol-2-yl)propanoate; (ii) the resulted methylic ester was converted to (RS)-2-(6-chloro-9H-carbazol-2-yl)propane hydrazide (carprofen hydrazide) by treatment with hydrazine hydrate; (iii) reaction of the hydrazid

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37

Markov, Andrey V., Aleksandra V. Sen’kova, Irina I. Popadyuk та ін. "Novel 3′-Substituted-1′,2′,4′-Oxadiazole Derivatives of 18βH-Glycyrrhetinic Acid and Their O-Acylated Amidoximes: Synthesis and Evaluation of Antitumor and Anti-Inflammatory Potential In Vitro and In Vivo". International Journal of Molecular Sciences 21, № 10 (2020): 3511. http://dx.doi.org/10.3390/ijms21103511.

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A series of novel 18βH-glycyrrhetinic acid (GA) derivatives containing 3′-(alkyl/phenyl/pyridin(-2″, -3″, and -4″)-yl)-1′,2′,4′-oxadiazole moieties at the C-30 position were synthesized by condensation of triterpenoid’s carboxyl group with corresponding amidoximes and further cyclization. Screening of the cytotoxicity of novel GA derivatives on a panel of tumor cell lines showed that the 3-acetoxy triterpenoid intermediates—O-acylated amidoxime 3a-h—display better solubility under bioassay conditions and more pronounced cytotoxicity compared to their 1′,2′,4′-oxadiazole analogs 4f-h (median IC

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38

Farah Smaysem and Ahmed Salim. "Synthesis and Characterization of Some Heterocyclic Compounds and Evaluation of Antibacterial Activity." International Journal of Research in Pharmaceutical Sciences 11, SPL4 (2020): 2068–78. http://dx.doi.org/10.26452/ijrps.v11ispl4.4421.

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In this study, heterocyclic compounds with two nitrogen atoms are prepared by reaction of 2-aminobenzimidazole with formic acid to get amide derivatives (A), reacts with phenylhydrazine to get phenyl hydrazone derivatives (B), reacts with ethyl chloroacetate to obtain ethyl acetate derivatives (C). The derivative (D) obtains on heating in a basic medium. The (B) reacts with 2-chloroacetyl chloride to give derivatives (E). A number of Schiff bases are prepared (F, I) from reacting 2-aminobenzimidazole with benzaldehyde derivatives. The(F) reacts with propargyl bromide to give propargyl bromide

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39

Journal, Baghdad Science. "Synthesis of New Heterocyclic Derivatives from 4-(3, 5-Dimethyl-1-phenyl-1H-pyrazol-4-ylazo)- benzoic acid." Baghdad Science Journal 7, no. 1 (2010): 727–36. http://dx.doi.org/10.21123/bsj.7.1.727-736.

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In this work pyrazolin derivatives were prepared from the diazonium chloride salt of 4-aminobenzoic acid. Azo compounds were prepared from the reaction of an ethanolic solution of sodium acetate and calculated amount of active methylene compound namely, acetyl acetone to obtain the corresponding hydrazono derivative (1). Cyclocondensation reaction of compounds (1) with hydrazine hydrate and phenyl hydrazine in boiling ethanol affording the corresponding pyrazoline-5-one derivatives of 4-aminobenzoic acid (2,3). Then compound (3) was reacted with thionyl chloride to give the corresponding acid

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40

Frederico Rozada, Andrew Matheus, Franciele Abigail Vilugron Rodrigues-Vendramini, Erika Seki Kioshima, et al. "Synthesis of 1,3,4-oxadiazoles with 4-methoxynaphthalene ring: discovering new compounds with antimicrobial activity." Future Medicinal Chemistry 15, no. 24 (2023): 2239–55. http://dx.doi.org/10.4155/fmc-2023-0153.

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Background: Paracoccidioidomycosis (PCM) is a systemic infection caused by Paracoccidioides spp. ( Pb). PCM can be associated or clinically confused with tuberculosis (TB), another pulmonary infection, caused by Mycobacterium tuberculosis ( Mtb). Futhermore, the long treatment time of TB and PCM and the cases of TB drug resistance impose difficulties for the cure of these diseases. Results: New 1,3,4-oxadiazoles containing the 4-methoxynaphthalene ring were synthesized and their antimicrobial activity was evaluated against Pb and Mtb. The derivative 6n (with 2-hydroxy-5-nitrophenyl subunit) is

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41

Huang, Mei Hua, Zong Fang Tian, and Hui Huang. "Synthesis and Photovoltaic Properties of Poly(p-phenylenevinylene) Derivatives Modified by Thiophene Derivatives." Advanced Materials Research 643 (January 2013): 13–16. http://dx.doi.org/10.4028/www.scientific.net/amr.643.13.

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Two novel conjugated polymers (P1 and P2), consisting of 2,5-dioctyloxy-1,4- phenylenevinylene and terthiophene derivative based on 3,4-ethylenedioxythiophene, named TTh-Oxa, with oxadiazole side chains, have been synthesized via the Witting–Horner reaction. Another poly(p-phenylene vinylene) (PPV) derivative P3 was also prepared for comparison. The introduction of TTh-Oxa unit in polymer benefits to widening and red shifting the absorption spectra of PPV derivatives. Photovoltaic cells were fabricated with the as-synthesized polymers as the donors and [6,6]-phenyl-C61-butyric acid methyl este

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42

Sanaryh Mohammed Al-awad, Leaqaa Abdalredha raheem, and Ausama Ayob Jaccob. "Synthesis and Pharmacological Evaluation of Novel Coumarin Derivatives." International Journal of Research in Pharmaceutical Sciences 11, no. 1 (2020): 865–74. http://dx.doi.org/10.26452/ijrps.v11i1.1908.

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The current work focuses on new architecture, synthesis of coumarin-oxadiazole hybrid derivative products as both these (coumarin ring and oxadiazole) have a wide variety of biological behavior, Compounds containing the nucleus of coumarin (2H-1-benzopyran-2-one) are an interesting class of hetero cycles which hold an important role in the field of natural ingredients and synthetic organic chemistry. It has been exciting medicinal chemists to study native coumarins or synthetic analogs for their application for decades. And they can be further modified to synthesize more effective and potent d

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43

Amir, Mohammad, and Shikha Kumar. "Synthesis and evaluation of anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation properties of ibuprofen derivatives." Acta Pharmaceutica 57, no. 1 (2007): 31–45. http://dx.doi.org/10.2478/v10007-007-0003-y.

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Synthesis and evaluation of anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation properties of ibuprofen derivatives In order to reduce the ulcerogenic effect of ibuprofen, its carboxylic group has been converted into 5-membered heterocyclic rings. Various 1,3,4-oxadiazoles (3-8, 16-21), 1,2,4-triazoles (22-27), 1,3,4-thiadiazoles (28-30), and 1,2,4-triazine (9) derivatives of ibuprofen were prepared by cyclization of 2-(4-i-butylphenyl) propionic acid hydrazide (2) and N1-[2-(4-i-butylphenyl) propionyl]-N4-alkyl/arylthiosemicarbazides (10-15) under various reaction conditions. The

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44

KUMAR, SURESH, VIKAS KALIA, and HARIOM DAHIYA. "Study of Anticorrosive Action and Synthesis of 2-(Phenoxymethyl)-5-p-tolyl- 1,3,4-oxadiazole in 1 M Hydrochloric Acid Medium for Mild Steel." Asian Journal of Chemistry 34, no. 3 (2022): 597–606. http://dx.doi.org/10.14233/ajchem.2022.23560.

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Oxadiazole derivative 2-(phenoxymethyl)-5-p-tolyl-1,3,4-oxadiazole (2POM5PTO) was prepared by condensation of phenoxymethyl hydrazine with p-tolualdehyde. Further tested as corrosion inhibitor for mild steel via electrochemical methods, potentiodynamic polarization (PDP) and gravimetric experiments. An increasing trend in inhibition efficiency has been seen on raising the concentration of 2POM5PTO. PDP technique reveals the mixed-type inhibitor behaviour of 2POM5PTO. The depressed semicircular Nyquist plot explains that the charge transfer resistance increased with inhibitor concentration whil

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45

Al-Sahib, Sanaa A., Sana Hitur Awad, and Khalida A. Thejeel. "Synthesis, Characterization Of Organic Nanoparticles of Oxadiazole Derivative." Journal of Physics: Conference Series 1294 (September 2019): 052024. http://dx.doi.org/10.1088/1742-6596/1294/5/052024.

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46

Ester, David, Declan McKearney, Khrystyna Herasymchuk, and Vance Williams. "Heterocycle Effects on the Liquid Crystallinity of Terthiophene Analogues." Materials 12, no. 14 (2019): 2314. http://dx.doi.org/10.3390/ma12142314.

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Liquid crystalline self-assembly offers the potential to create highly ordered, uniformly aligned, and defect-free thin-film organic semiconductors. Analogues of one of the more promising classes of liquid crystal semiconductors, 5,5”-dialkyl-α-terthiophenes, were prepared in order to investigate the effects of replacing the central thiophene with either an oxadiazole or a thiadiazole ring. The phase behaviour was examined by differential scanning calorimetry, polarized optical microscopy, and variable temperature x-ray diffraction. While the oxadiazole derivative was not liquid crystalline, t

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47

Paswan, Santosh, Manoj K. Bharty, Sanyucta Kumari, Sushil K. Gupta, and Nand K. Singh. "Crystal structure of 5-(furan-2-yl)-N-phenyl-1,3,4-oxadiazol-2-amine." Acta Crystallographica Section E Crystallographic Communications 71, no. 11 (2015): o880—o881. http://dx.doi.org/10.1107/s2056989015019453.

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The title compound, C12H9N3O2, was obtained as a cyclized oxadiazole derivative from substituted thiosemicarbazide in the presence of manganese(II) acetate. The furan ring is disordered over two orientations, with occupancies of 0.76 (2) and 0.24 (2). The dihedral angles between the central oxadiazole ring and the pendant phenyl ring and furan ring (major disorder component) are 3.34 (18) and 5.7 (6)°, respectively. A short intramolecular C—H...O contact generates anS(6) ring. In the crystal, inversion dimers linked by pairs of N—H...N hydrogen bonds generateR22[8] loops. The dimers are linked

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48

El-Sayed, Wael A., Farag A. El-Essawy, Omar M. Ali, Barsis S. Nasr, Mohamed M. Abdalla, and Adel A. H. Abdel-Rahman. "Anti-HIV Activity of New Substituted 1,3,4-Oxadiazole Derivatives and their Acyclic Nucleoside Analogues." Zeitschrift für Naturforschung C 64, no. 11-12 (2009): 773–78. http://dx.doi.org/10.1515/znc-2009-11-1203.

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A number of new 5-[(naphthalen-5-yloxy)methyl]-1,3,4-oxadiazole derivatives, 2 - 5 and 8 - 11, were synthesized. The 2-{5-[(naphthalen-5-yloxy)methyl]-1,3,4-oxadiazol-2-ylthio}acetohydrazones 6a and 6b were synthesized by the reaction of the hydrazide 4 with the corresponding monosaccharides. Cyclization of the sugar hydrazones 6a and 6b with acetic anhydride afforded the substituted oxadiazoline derivatives 7a and 7b. The synthesized compounds were evaluated for their antiviral activity against, the human immunodefi ciency virus (HIV-1) and some of these compounds showed moderate to high anti

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49

Lhoták, Pavel, and Antonín Kurfürst. "Synthesis of Luminophoric Derivatives of PBD Based on 2,5-Diaryl Substituted Thiazoles and Oxazoles." Collection of Czechoslovak Chemical Communications 58, no. 11 (1993): 2720–28. http://dx.doi.org/10.1135/cccc19932720.

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The Friedel-Crafts acylation of 2-(biphenyl-4-yl)-5-phenyl-1,3,4-oxadiazole (PBD) with hippuryl chloride has been used to prepare the derivative V which on cyclization with POCl3 or P4S10 gives the respective oxazole (or thiazole) derivative of PBD, XIa or XIb. The reaction of carboxylic acid II with 4-(o-aminoacetyl)biphenyl in the presence of CDI gives N-acyl-α-aminoketone VII; the analogous compound VI has been prepared by acylating of o-aminoacetophenone with acyl chloride III. The cyclization of these compounds gives bifluorophores Xa - Xd.

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50

Alkhaldi, Abdulsalam A. M., Mohamed A. Abdelgawad, Bahaa G. M. Youssif, Ahmed O. El-Gendy, and Harry P. De Koning. "Synthesis, antimicrobial activities and GAPDH docking of novel 1, 2, 3-triazole derivatives." Tropical Journal of Pharmaceutical Research 18, no. 5 (2021): 1101–8. http://dx.doi.org/10.4314/tjpr.v18i5.27.

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Purpose: To synthesize new triazole derivatives in order to overcome the problem of side effects of antimicrobial agents and microbial resistance, while broadening the spectrum of antimicrobial activity. Methods: The starting triazole, compound 1, was prepared through click chemistry and reacted with chloroacetyl chloride to yield compound II. Triazole 1 was reacted with acids and aldehydes to produce oxadiazole (III) and azomethine (IV) which cyclized in acetic anhydride to give a new acetylated oxadiazole (V). Minimum inhibitory concentration (MIC) and resorufin assays were used for an

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