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Journal articles on the topic '4-Oxadiazole derivatives'

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Published: 4 June 2025

Last updated: 1 August 2025

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1

Solet, Sanwar Mal, Neetesh Kumar Sharma, and Raghvendra Singh Bhadauria. "Synthesis of 2, 5-disubstituted-1, 3, 4-oxadiazole derivatives." Journal of Drug Delivery and Therapeutics 9, no. 4-A (2019): 528–60. http://dx.doi.org/10.22270/jddt.v9i4-a.3514.

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Synthesis of a series of various 2, 5-disubstituted-1, 3, 4-oxadiazole derivatives (7a-7u) have been done. Synthesis of a series of intermediates (3a-3c and 5a-5c) have been also done, ethyl-2-phenoxyacetate (3a), ethyl 2-(2, 4-dichlorophenoxy)acetate (3b), ethyl 2-(4-nitrorophenoxy) acetate (3c), 2-phenoxyacetohydrazide (5a), 2-(2, 4-dichlorophenoxy) acetohydrazide (5b), 2-(4-nitrophenoxy)acetohydrazide (5c), and final product (7a-7u), 2-(phenoxymethyl)-5-phenyl-1, 3, 4-oxadiazole (7a), 4-(5-(phenoxymethyl)-1, 3, 4-oxadiazol-2-yl)aniline (7b), 3-(5-(phenoxymethyl)-1, 3, 4-oxadiazol-2-yl) anil

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2

Solet, Sanwar Mal, Neetesh Kumar Sharma, and Raghvendra Singh Bhadauria. "Biological Evaluation of Novel Synthesized 2, 5-disubstituted-1, 3, 4-oxadiazole derivatives." Journal of Drug Delivery and Therapeutics 9, no. 4-A (2019): 573–76. http://dx.doi.org/10.22270/jddt.v9i4-a.3522.

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Synthesis of a series of various 2, 5-disubstituted-1, 3, 4-oxadiazole derivatives (7a-7v) have been done previously. These novel synthesized derivatives (7a-7v) have been tested for their antibacterial activity against Gram +ve S. aureus and Gram -ve E. Coli bacterias by broth dilution method. A comparative study has been done for all derivatives. Based on the visual turbidity, the MIC of the evaluated molecules has been studied, the evaluation concentration was used single therefore, the exact MIC could not determined and results are represented in less than and more than based on growth of

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3

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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4

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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5

R., Sapthagiri, Sriram R., Ilavarasan L., and Ravi A. "SYNTHESIS AND CHARACTERIZATION OF 2-AMINO-1, 3, 4-OXODIAZOLE DERIVATIVES." International Journal of Applied and Advanced Scientific Research 1, no. 2 (2017): 61–65. https://doi.org/10.5281/zenodo.258975.

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A simple protocol for the synthesis of 2-amino-1, 3, 4-oxadiazole derivatives using iodoaceticacid as a cyclodesulfurization agent. This method is also applicable to the synthesis of various substituted 2-amino-1, 3, 4-oxadiazole derivatives such as 5-(2-bromophenyl)-N-phenyl-1, 3, 4-oxadiazol-2-amine. The synthesized methodology was simple and hazardless, it’s giving good yield.

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6

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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7

Bandeira, Gustavo Neto, Claudio Augusto Gomes da Camara, Marcílio Martins de Moraes, João Paulo Ramos de Melo, João Rufino de Freitas Filho, and Jucleiton José Rufino de Freitas. "Synthesis and Insecticidal Activity of 1,2,4-Oxadiazoles Derivates against (Plutella xylostella L.) Diamondback Moth." Archives of Current Research International 25, no. 1 (2025): 283–92. https://doi.org/10.9734/acri/2025/v25i11058.

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The diamondback moth (Plutella xylostella) is a cosmopolitan pest known for its destruction of cruciferous plants. Commercial insecticides, such as Decis 25 EC and Azamax, are the main forms of controlling this pest in irrigated systems in the agricultural communities of the city of Garanhuns (northeastern Brazil). However, the difficulty in controlling this pest resides in its high fecundity and short lifecycle, which serve as resistance mechanisms to insecticides. Considering the immediate need to find alternative products to insecticides employed in these agricultural communities, nine 1,2,

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8

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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9

Saini, Sachin. "Synthesis and Anticonvulsant Studies of Thiazolidinone and Azetidinone Derivatives from Indole Moiety." Drug Research 69, no. 08 (2018): 445–50. http://dx.doi.org/10.1055/a-0809-5098.

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Abstract2-Amino-5-(3’-indolomethylene)-1, 3 , 4 - oxadiazole (3) undergoes facile condensation with various aromatic aldehydes to gave 2-substitiuted arylidenylamino-5-(3’- indolomethylene) – 1, 3 , 4 – oxadiazole (4–8). Cyclocondensation of (4–8) with thioglycolic acid and triethylamine yielded 3-[5’-(3”- indolomethylene)- 1’, 3’, 4’- oxadiazol-2’-yl]- 2- (substituted aryl)-4- thiazolidinones (9–13) and 1-[5’-(3”- indolomethylene) -1’, 3’, 4’- oxadiazol - 2’- yl ] -4-(substituted aryl) -2- azetidinones (14–18). The structures of these compounds were established on the basis of analytical and

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10

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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Nikita, Gaikwad*1 Dinesh Kawade2 Dhananjay Tidke3 Shubham Khandare4 Sneha Nandeshwar5. "Heterocyclic 1, 3, 4-Oxadiazole Compounds with Diverse Biological Activities - A Comprehensive Review." International Journal of Pharmaceutical Sciences 2, no. 12 (2024): 1324–34. https://doi.org/10.5281/zenodo.14378794.

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1,3,4-oxadiazoles, heterocycles bearing one oxygen and two nitrogen atoms in a five membered ring have their application in the diverse areas of medicine.[1] This interesting group of compounds has diverse biological activities such as antibacterial, antifungal, antiviral, anticonvulsant, anticancer, anti-inflammatory, anti HIV, anti-tubercular  activity etc.[2] Researchers  are interested in developing and studying novel heterocyclic compounds that contain 1,3,4-oxadiazole because of its many significant applications. We have attempted to provide an overview of some of the significa

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12

Górecki, Sebastian, and Agnieszka Kudelko. "Synthesis and Characterization of Novel 2-Alkyl-1,3,4-Oxadiazoles Containing a Phenylazo Group." Molecules 29, no. 18 (2024): 4316. http://dx.doi.org/10.3390/molecules29184316.

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An efficient method for the synthesis of novel phenylazo-containing moieties is described. The derivatives of 5-(4-(phenyldiazenyl)phenyl)-1,3,4-oxadiazole, substituted at position 2 of the heterocyclic scaffold with alkyl groups of different chain lengths, were prepared. The titled compounds were obtained using the appropriate 4-(5-alkyl-1,3,4-oxadiazol-2-yl)anilines, which were directed to diazotization and subsequently coupled to phenol, resorcinol, and N,N-dimethylaniline. Additionally, we report a mild and effective procedure for the preparation of 4-(5-alkyl-1,3,4-oxadiazol-2-yl)anilines

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13

Lata, Suman, Lucky Choudhary, Komalpreet Kaur, Shivani Bharti, and Vikrant Abbot. "Synthesis of 4-hydroxy-2H-chromene-2-one and 1,3,4-oxadiazole hybrids as potential antioxidant and antibacterial agents." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 35, no. 02 (2025): 385. https://doi.org/10.59467/ijhc.2025.35.385.

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A new series of 4-hydroxy-3-(2-(5-phenyl-1,3,4-oxadiazol-2-ylamino)ethyl)-2H-chromen-2-one derivatives (4a-4e) was synthesized by the hybrid approach and evaluated for antioxidant and antibacterial activity. The antibacterial results revealed that derivatives 4d and 4e exhibited superior activity compared to ciprofloxacin, a commonly used standard antibacterial agent. These findings highlight the promising pharmacological profile of the synthesized coumarin-oxadiazole hybrids, particularly as potent antibacterial and antioxidant agents, which warrants further investigation for potential therap

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14

Farah, Deeba, Abbas Naeem, Tahir Butt Muhammad, Ahmad Khan Rauf, Muneeb Ahsan Muhammad, and Ain Khan Misbahul. "Synthesis, characterization and biological activities of 1,3,4-oxadiazole derivatives of nalidixic acid and their copper complexes." Chemistry International 4, no. 4 (2018): 206–15. https://doi.org/10.5281/zenodo.1475387.

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A series of novel 1, 3, 4-oxadiazole analogues was synthesized from cyclization of hydrazones of substituted 1-ethyl-1,4-dihydro-7-methyl-4-oxo-1,8-naphthyridine-3-carbohydrazides were prepared from nalidixic acid. The structures of synthesized oxadiazole derivatives and their copper complexes were elucidated on the basis of FTIR, elemental analyses, 1H-NMR and atomic absorption spectral analysis. It was observed from spectral data that metal ligand ratio was 1:1 in all copper complexes and they were bidentate, coordination was found to be done through oxygen of 4-oxo group and nitrogen of oxa

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15

Nisheeth, Rastogi, and Anil Harrison Darwin. "Synthesis and antifungal activity of some new derivatives of 5-{ 4' -(2" ,4"- dichlorobenzyloxy)-phenyl }-1 ,3,4-oxadiazole-2(3H)-thione." Journal of Indian Chemical Society Vol. 89, Nov 2012 (2012): 1543–50. https://doi.org/10.5281/zenodo.5771647.

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Department of Chemistry, Lucknow Christian Post-Graduate College, Lucknow-226 018, Uttar Pradesh, India <em>E-mail </em>: nisheethrastogi2003@gmail.com <em>Manuscript received 06 June 2011, revised OJ February 2012, accepted 08 February 2012</em> 5-{ 4'-(2" ,4" -Dichlorobenzyloxy)-phenyl}-1,3,4-oxadiazole-2(3<em>H</em>)-thione (2) was prepared by the reaction of 4- (2' ,4' -dichlorobenzyloxy)-benzoylhydrazine (1) with potassium isopropylxanthate in isopropyl alcohol. 5-{ 4' -(2" ,4"- Dichlorobenzyloxy)-phenyl}-1,3,4-oxadiazole-2(3<em>H</em>)-thione (2) on be

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16

Variya, Hiren H., Vikram Panchal, Falguni G. Bhabhor, and G. R. Patel. "Synthesis and Characterization of Biologically Potent Chalcone Bearing 1,3,4-Oxadiazole Linkage." International Letters of Chemistry, Physics and Astronomy 61 (November 2015): 77–83. http://dx.doi.org/10.18052/www.scipress.com/ilcpa.61.77.

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In this article, we have described to design and synthesized a series of substituted chalcone based 1,3,4-oxadiazole derivatives. Titled compounds (E)-S-(-5-phenyl-1,3,4-oxadiazol-2-yl) 2-(4-(3-(5-methyl-3oxo-2(p-tolyl)-2,3-dihydro-1H-pyrazol-4-yl)-3-oxoprop-1-en-1-yl) phenoxy) etanethioate (III1-6) were synthesized using of derivatives of S-(-5-phenyl-1,3,4 oxadiazole-2-yl)2-chloroethaethioate (I1-6) were reacted with (E)-4-(3-(4-hydroxyphenyl) acryloyl)-5-methyl-2(p-tolyl)-1H-pyrazol-3(2H)-one (II) in presence of K2CO3 in DMF as a solvent. The synthesized compounds were evaluated for their a

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Variya, Hiren H., Vikram Panchal, Falguni G. Bhabhor, and G. R. Patel. "Synthesis and Characterization of Biologically Potent Chalcone Bearing 1,3,4-Oxadiazole Linkage." International Letters of Chemistry, Physics and Astronomy 61 (November 3, 2015): 77–83. http://dx.doi.org/10.56431/p-x4q61z.

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In this article, we have described to design and synthesized a series of substituted chalcone based 1,3,4-oxadiazole derivatives. Titled compounds (E)-S-(-5-phenyl-1,3,4-oxadiazol-2-yl) 2-(4-(3-(5-methyl-3oxo-2(p-tolyl)-2,3-dihydro-1H-pyrazol-4-yl)-3-oxoprop-1-en-1-yl) phenoxy) etanethioate (III1-6) were synthesized using of derivatives of S-(-5-phenyl-1,3,4 oxadiazole-2-yl)2-chloroethaethioate (I1-6) were reacted with (E)-4-(3-(4-hydroxyphenyl) acryloyl)-5-methyl-2(p-tolyl)-1H-pyrazol-3(2H)-one (II) in presence of K2CO3 in DMF as a solvent. The synthesized compounds were evaluated for their a

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18

Kumar, Davinder, Navidha Aggarwal, Virender Kumar, et al. "Synthesis, Anticancer, Antimicrobial and Antioxidant Potential of Novel 4-(Substituted phenyl-1,3,4-oxadiazol/thiadiazol-2-yl)-4-(4-substituted phenyl) Azetidin-2-One Derivatives." Pharmaceuticals 16, no. 4 (2023): 517. http://dx.doi.org/10.3390/ph16040517.

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By exploiting the ample biological potential of 1,3,4-oxadiazole/thiadiazole ring, 4-substitutedphenyl-1,3,4-oxadiazol/Thiadiazol-2-yl)-4-(4-substitutedphenyl) azetidin-2-one derivatives were prepared. Various substituted azetidin-2-one derivatives have been identified as immunostimulating and antimicrobial, as well as their antioxidant activity. 2-amino 1,3,4 oxadiazole/thiadiazole conjugates were synthesized by mixing semi/thio carbazides and sodium acetate with water and stirring well, followed by adding aldehydes in methanol at room temperature. Acetate (glacial) was used as the catalyst t

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19

Deeksha Tiwari, Rakesh Narang, and Sukhbir Lal khokra. "A review on microwave assisted synthesis, mechanism of action and structure activity relationship of 1, 3, 4-oxadiazoleA review on microwave assisted synthesis, mechanism of action and structure activity relationship of 1, 3, 4-oxadiazole derivatives as anticancer agent derivatives as anticancer agent." World Journal of Advanced Research and Reviews 9, no. 1 (2021): 086–96. http://dx.doi.org/10.30574/wjarr.2021.9.1.0472.

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1, 3, 4-oxadiazole derivatives received considerable attention of different research groups, as they have wide variety of biological activities. 1, 3, 4-oxadiazole derivatives exhibited noteworthy anticancer activities. In recent years, microwave-induced organic reactions attained significant attention due to several benefits, such as short reaction time, cost-effectiveness, excellent yield, and ease of work. In view of above in present work, SAR and mechanism of action of 1, 3, 4-oxadiazole derivatives as anticancer agents, reported by different research groups in recent years are summarized.

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Deeksha, Tiwari, Narang Rakesh, and Lal khokra Sukhbir. "A review on microwave assisted synthesis, mechanism of action and structure activity relationship of 1, 3, 4-oxadiazole derivatives as anticancer agent." World Journal of Advanced Research and Reviews 9, no. 1 (2021): 086–96. https://doi.org/10.5281/zenodo.4533782.

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1, 3, 4-oxadiazole derivatives received considerable attention of different research groups, as they have wide variety of biological activities. 1, 3, 4-oxadiazole derivatives exhibited noteworthy anticancer activities. In recent years, microwave-induced organic reactions attained significant attention due to several benefits, such as short reaction time, cost-effectiveness, excellent yield, and ease of work. In view of above in present work, SAR and mechanism of action of 1, 3, 4-oxadiazole derivatives as anticancer agents, reported by different research groups in recent years are summarized.

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21

S. Ahmed, Wurood, Ammar A. Razzak Mahmood, and Redha I. Al-Bayati. "Synthesis and Evaluation of Antimicrobial Activity of New Imides and Schiff Bases Derived from Ethyl -4-Amino Benzoate." Oriental Journal of Chemistry 34, no. 5 (2018): 2477–86. http://dx.doi.org/10.13005/ojc/340533.

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A series of disubstituted 1,3,4-oxadiazole derivatives, including imides and Schiff bases, was achieved from the starting material, ethyl-4-aminobenzoate, which was converted to the corresponding 4-aminobenzohydrazide (1), by its reaction with hydrazine hydrate in absolute ethanol. Two oxadiazole parent nuclei had been synthesized from (1), the first nucleus 5-(4-aminophenyl)-1,3,4-oxadiazol-2-amine(2), and the second is 5-(4-aminophenyl)-1,3,4-oxadiazole-2-thione (3). Compound (2) Obtained from stirring methanolic solution of (1) with cyanogen bromide (CNBr) and sodium bicarbonate (NaHCO3) at

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R., N. VANSDADIA, J. VIKANI H., and RAREKH HANSA. "Studies on 1,3,4-Oxadiazoles. Part-XII. Preparation and Antimicrobial Activity of p,p'-Bis(2-substituted-benzalamino/benzoylamino-1,3,4-oxadiazol-5-ylmethoxy)diphenyl Sulphones." Journal of Indian Chemical Society Vol. 65, Nov 1988 (1988): 782–83. https://doi.org/10.5281/zenodo.6090174.

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Department of Chemistry, Saurashtra University, Rajkot-860 005 <em>Manuscript received 16 May 1988, accepted 2 .August 1988</em> <em>p,p'</em>-Bis(hydrazinocarbonylmethoxy)diphenyl sulphone (1) was treated with cyanogen bromide to get<em> p,p'</em>-bis(2-amino-1,3,4-oxadiazol-5-ylmethoxy)diphenyl sulphone (2) which was condensed with different aromatic aldehydes/acid chlorides to get the corresponding benzalamino (3)/benzoylamino (4)-oxadiazole derivatives.

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Wołek, Barbara, Mateusz Werłos, Magdalena Komander, and Agnieszka Kudelko. "Efficient Synthesis of Novel 1,3,4-Oxadiazoles Bearing a 4-N,N-Dimethylaminoquinazoline Scaffold via Palladium-Catalyzed Suzuki Cross-Coupling Reactions." Molecules 25, no. 21 (2020): 5150. http://dx.doi.org/10.3390/molecules25215150.

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Two series of novel (symmetrical and unsymmetrical) quinazolinylphenyl-1,3,4-oxadiazole derivatives were synthesized using palladium-catalyzed Suzuki cross-coupling reactions. The presented synthetic methodology is based on the use of bromine-substituted 2-phenyl-4-N,N-dimethylaminoquinazolines and either a boronic acid pinacol ester or a diboronic acid bis(pinacol) ester of 2,5-diphenyl-1,3,4-oxadiazole. The reactions are conducted in a two-phase solvent system in the presence of catalytic amounts of [1,1′-bis(diphenylphosphino)ferrocene]-dichloropalladium(II), sodium carbonate, and tetrabuty

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Kaya, Betül, Weiam Hussin, Leyla Yurttaş, et al. "Design and Synthesis of New 1,3,4-Oxadiazole – Benzothiazole and Hydrazone Derivatives as Promising Chemotherapeutic Agents." Drug Research 67, no. 05 (2017): 275–82. http://dx.doi.org/10.1055/s-0042-119070.

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AbstractLooking for new cytotoxic and antimicrobial agents with improved antitumor activity, a series of hydrazide and oxadiazole derivatives were designed and synthesized using 3-methoxyphenol as starting substance. Novel N’-(arylidene)-2-(3-methoxyphenoxy)acetohydrazide derivatives (4a–f)/1-(4-substitutedphenyl)-2-[(5-[(3-methoxyphenoxy)methyl]-1,3,4-oxadiazol-2-yl)thio]ethan-1-one derivatives (6a–f)/N-(6-substitutedbenzothiazol-2-yl)-2-[(5-[(3-methoxyphenoxy)methyl]-1,3,4-oxadiazol-2-yl)thio]acetamide derivatives (7a–e) were obtained and evaluated for their in vitro antimicrobial activity a

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Gatphoh, Banylla Felicity Dkhar, Natasha Naval Aggarwal, S. Madan Kumar, M. Vijay Kumar, and B. C. Revanasiddappa. "Synthesis, in silico analysis and antidepressant activity of 1,3,4-oxadiazole derivatives." Bangladesh Journal of Pharmacology 17, no. 1 (2022): 14–21. http://dx.doi.org/10.3329/bjp.v17i1.58728.

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The compounds 1,3,4-oxadiazole derivatives (1-8) were synthesized by the cyclization of 4-hydroxy benzhydrazide (1) with various substituted aroma-tic aldehydes (2) using FeCl3 as catalyst and methanol as a solvent medium. The structures of the newly synthesized compounds were assigned based on FT-IR, 1H-NMR, and mass spectral data. In vivo antidepressant activity was performed by tail suspension test and forced swimming test models. Using the Schrodinger Maestro, the in silico analysis was performed and docked to the glycogen synthase kinase 3β binding site (PDB: 3GB2). Compounds 8 [4,4'-(1,3

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Nguyen Tien, Cong, Duc Tran Thi Cam, Ha Bui Manh, and Dat Nguyen Dang. "Synthesis and Antibacterial Activity of Some Derivatives of 2-Methylbenzimidazole Containing 1,3,4-Oxadiazole or 1,2,4-Triazole Heterocycle." Journal of Chemistry 2016 (2016): 1–6. http://dx.doi.org/10.1155/2016/1507049.

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5-[(2-Methyl-1H-benzimidazol-1-yl)methyl]-1,3,4-oxadiazole-2-thiol or 5-[(2-methyl-1H-benzimidazol-1-yl)methyl]-4-(4-methylphenyl)-1,2,4-triazol-3-thiol which were prepared starting from 2-methylbenzimidazole in the reaction with appropriateN-aryl-2-chloroacetamides afforded two series ofN-aryl-2-{5-[(2-methyl-1H-benzimidazol-1-yl)methyl]-1,3,4-oxadiazol-2-yl}sulfanylacetamides andN-aryl-2-{5-[(2-methyl-1H-benzimidazol-1-yl)methyl]-4-(4-methylphenyl)-4H-1,2,4-triazol-3-ylthio}acetamides, respectively. The structures of the compounds were elucidated on the basis of IR, MS,1H-NMR, and13C-NMR spe

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Zhou, Ying, S. Y. Feng, and D. H. Zhang. "A probe molecule based on 1,3,4-oxadiazole was constructed for crystal structure analysis and Sn4+ identification." Журнал структурной химии 65, no. 11 (2024): 135435. http://dx.doi.org/10.26902/jsc_id135435.

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In order to develop the application of 1,3, 4-oxadiazole compounds in the direction of fluorescent probes, this paper modified the probes by introducing 2-(bromomethyl) pyridine on the amino group of 1,3, 4-oxadiazole derivatives, and synthesized HL1(2-(5-(2-aminophenyl)-1,3,4-oxadiazol-2-yl)-N-(pyridin-2-ylmethyl)aniline). Its structure was characterized by NMR, HRMS and single crystal X-ray diffraction. The weak interaction of HL1 was analyzed by using Multiwfn to draw Hirshfeld surface. The HOMO and LUMO orbitals of HL1 were analyzed in B3LYP/ 6-311++ G basis set using DFT theory. HL1 is hi

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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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Vachhani, Mukeshkumar, Jaydeep Lalpara, Sanjay Hadiyal, and Gaurang Dubal. "Microwave-assisted synthesis of bioactive tetrahydropyrimidine derivatives as antidiabetic agents." Folia Medica 64, no. 3 (2022): 478–87. http://dx.doi.org/10.3897/folmed.64.e62476.

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Abstract Introduction: In drug discovery, pyrimidine analogues show good biological response and many drug moieties have pyrimidine core. Aim: On the basis of prior review, we synthesized a series of N-(substituted phenyl)-1,3,6-trimethyl-4-(4-((5-(4-nitrophenyl)-1,3,4-oxadiazol-2-yl)methoxy)phenyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide parade a 1,3,4-oxadiazole core which were evaluated for in vitro antidiabetic screening. Materials and methods: The tetrahydropyrimidine derivatives have been synthesized by microwave irradiation method. It was carried out by Biginelli condensation o

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Manojkumar, Parameswaran, Thengungal Ravi, and Gopalakrishnan Subbuchettiar. "Synthesis of coumarin heterocyclic derivatives with antioxidant activity and in vitro cytotoxic activity against tumour cells." Acta Pharmaceutica 59, no. 2 (2009): 159–70. http://dx.doi.org/10.2478/v10007-009-0018-7.

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Synthesis of coumarin heterocyclic derivatives with antioxidant activity andin vitrocytotoxic activity against tumour cellsThe aim of the present work was to synthesise coumarinyl heterocycles and to elucidate the potential role of these compounds as antioxidants and cytotoxic agents against Dalton's lymphoma ascites tumour cells (DLA) and Ehrlich ascites carcinoma cells (EAC). The synthesis of coumarin derivatives containing pyrazole, pyrazolone, thiazolidin-4-one, 5-carboxymethyl-4-thiazolidinone and 3-acetyl-1,3,4-oxadiazole ring is reported. 4-Methylcoumarinyl-7-oxyacetic acid hydrazide (1

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Abdukhakim, A. Ziyaev, F. Tozhiev Ibodylla, A. Sasmakov Sobirdjan, S. Azimova Shahnoz, Zh. Elmuradov Burkhon, and S. Ismailova Dilnoza. "Selective s-alkoxycarbonylation of isomeric 5-pyridyl-1,3,4-oxadiazoles and antimicrobial activity of the synthesized compounds." Pharmaceutical and Chemical Journal 4, no. 2 (2017): 29–34. https://doi.org/10.5281/zenodo.13762644.

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Selective S-alkoxycarbonylation of isomeric - 5-(2-pyridyl)- (<strong>1</strong>), 5-(3-pyridyl)- (<strong>2</strong>), and 5-(4-pyridyl)-1,3,4-oxadiazol-2-thiones (<strong>3</strong>)<strong> </strong>have been studied and novel series of S-substituted derivatives (<strong>7-15</strong>) have been synthesized and characterized by physical methods of research. No formation of the amides - N-substituted derivatives (<strong>A</strong>) was observed. The antimicrobial tests indicated that the 2-alkyloxycarbonylthio-oxadiazole derivatives exhibited a remarkable activity against Gram-positive bact

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32

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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33

Santhanalakshmi, K., K. Margandan, P. Manivannan, and Rosy P. Jacquline. "Pharmacological significance of Oxadiazole scaffold." Research Journal of Chemistry and Environment 25, no. 8 (2022): 177–88. http://dx.doi.org/10.25303/258rjce177188.

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Heterocycles come under an important branch of organic chemistry that contains at least one atom other than carbon as a part of ring system. The most common hetero atoms that are widely used are nitrogen, oxygen and sulphur. In synthetic organic chemistry, synthesis of heterocyclic compound is of immense interest due to its therapeutic applications and their existence in several natural products like vitamins, hormones, antibiotics and alkaloids. The oxadiazole nucleus is one of the most significant and well known heterocyclic compounds due to its broad range of pharmacological and therapeutic

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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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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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Ramesh, Aswathy, Rakesh Kumar Jat, and R. Arunkumar. "Pharmacological Evaluation of Novel 1,3,4-Oxadiazole Derivatives." International Journal of Medical Sciences and Pharma Research 10, no. 1 (2024): 26–34. http://dx.doi.org/10.22270/ijmspr.v10i1.88.

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A series of 2, 5- disubstituted- 1, 3, 4-oxadiazole derivatives (Ox1-Ox10) are synthesized by the ring condensation reaction followed by rearrangement of salicylic acid and phenyl acetic acid with various aromatic acids in presence of phosphorous oxychloride as cyclizing agent. Structure of the new derivatives are confirmed by spectral analysis. Those derivatives having high Pa value in PASS software are subjected to antibacterial, anticancer and antidiabetic studies which yield promising reports. This study helps and stimulate the researcher to exploit the oxadiazole nuclei for the developmen

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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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38

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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39

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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40

Sonu Jangir, Sonu Jangir, and Satish Satish. "“A Design and Synthesis of Some New 1, 3, 4-Oxadiazole Analogues for Using Anticancer Agents”." International Journal of Pharmaceutical Research and Applications 10, no. 3 (2025): 1248–67. https://doi.org/10.35629/4494-100312481267.

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The abstract of the design and synthesis of 1,3,4- oxadiazole analogues as anticancer agents discusses the creation of new compounds with potential anticancer properties. The study focused on developing 1, 3, 4-oxadiazole derivatives as promising agents against cancer. These derivatives were designed and synthesized, aiming to enhance their cytotoxicity against various cancer cell lines. The development of novel anticancer agents with improved efficacy and reduced toxicity is a pressing need in cancer research. In this study, we report the design, synthesis, of a series of 1,3,4- Oxadiazole an

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Jadhav, Pooja Subhash, Dipali Pandharinath Gadekar, Prerana B. Jadhav, and Shailaja B. Jadhav. "Design, molecular docking studies and ADME prediction of 2, 5-disubstituted 1, 3, 4-oxadiazole derivatives as CYP51 inhibitor for antimicrobial activity." Current Trends in Pharmacy and Pharmaceutical Chemistry 4, no. 2 (2022): 83–89. http://dx.doi.org/10.18231/j.ctppc.2022.015.

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The 1, 3, 4-Oxadiazole nucleus offers a wide range of applications in hetero cyclic chemistry, including antimicrobial medicine. A series of the 2, 5-disubstituted 1, 3, 4-Oxadiazole derivatives were designed and study was performed against the ergosterol biosynthesis as an antimicrobial target. The drug-likeness properties of the designed compounds were predicted. All the designed compounds showed good ADME properties and investigated for CYP51 inhibitory activity. According to molecular docking studies, all compounds showed better interaction with target protein and could be the potent inhib

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FT, Veneetha, Krishna KL, Monisha Harini S, and Vishwanathan B. "Assessment of 1, 3, 4- Oxadiazole Derivatives for Memory Enhancing Activity." International Journal of Pharma Research and Health Sciences 7, no. 2 (2019): 2942–47. http://dx.doi.org/10.21276/ijprhs.2019.02.04.

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Wang, Lei, Yu-Ran Wu, Shu-Ting Ren, et al. "Synthesis and bioactivity of novel C2-glycosyl oxadiazole derivatives as acetylcholinesterase inhibitors." Heterocyclic Communications 24, no. 6 (2018): 333–38. http://dx.doi.org/10.1515/hc-2018-0166.

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Abstract A series of glycosyl-substituted 1,3,4-oxadiazoles were synthesized by cyclization of glycosyl-acylthiosemicarbazides via a base-catalyzed reaction. The starting glycosyl-acylthiosemicarbazide derivatives were obtained by the reaction of glycosyl isothiocyanate with various hydrazides. The acetylcholinesterase (AChE) inhibitory activities of the products were tested by Ellman’s method. The most active compounds were subsequently evaluated for the 50% inhibitory concentration (IC50) values. N-(1,3,4,6-tetra-O-benzyl-2-deoxy-β-D-glucopyranosyl)-5-(4-fluorophenyl)-1,3,4-oxadiazole-2-amin

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44

Nakra, Vinod Kumar, and Manoj Sharma. "SYNTHESIS, CHARECTERIZATION AND ANTI-MICROBIAL ACTIVITY OF SUBSTITUTED 5-(5-SULFANYL-1,3,4-OXADIAZOL-2-YL)BENZENE- 1,2,3-TRIOL DERIVATIVES." Journal of Drug Delivery and Therapeutics 9, no. 4 (2019): 357–65. http://dx.doi.org/10.22270/jddt.v9i4.3060.

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A solution of propyl gallate(0.01 mol) in ethanol and hydrazine hydrate (0.01 mol) was refluxed for 4 hours. The excess solvent was distilled off under reduced pressure. The cooled residual mass was washed with distilled water. It was filtered and dried. The crude product was recrystallised from methanol to yield galloylhydrazide, Carbon disulfide (2 ml) was added drop wise to an ice cooled solution of KOH (2g) in ethanol (20 ml) containing the acid hydrazide 4 (0.02 mole), then the reaction mixture was stirred at room temperature 2h . After dilution with ethanol the solid precipitated was was

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Yurttaş, Leyla, Betül K. Çavuşoğlu, Gülşen A. Çiftçi, and Halide E. Temel. "Synthesis and Biological Evaluation of New 1,3,4-Oxadiazoles as Potential Anticancer Agents and Enzyme Inhibitors." Anti-Cancer Agents in Medicinal Chemistry 18, no. 6 (2018): 914–21. http://dx.doi.org/10.2174/1871520618666180322123327.

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Background: 1,3,4-Oxadiazoles have been known with a wide variety of pharmacological activities including anticancer activity. Objective: In this study, novel 2,5-disubstituted 1,3,4-oxadiazole derivatives were synthesized and evaluated for determining their anticancer, anticholinesterase and lipoxygenase (LOX) inhibitory activity. Methods: All compounds were tested against C6 rat glioma, A549 human lung carcinoma and NIH/3T3 mouse embryo fibroblast cell lines to define cytotoxic concentrations and apoptosis induction levels which they cause. Results: Many of the compounds exhibited remarkable

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46

SarveAhrabi, Yasin. "Anti-Helicobacter pylori Activity of New Derivatives of 1, 3,4-Oxadiazole: In Silico Study." Avicenna Journal of Clinical Microbiology and Infection 8, no. 4 (2021): 135–38. http://dx.doi.org/10.34172/ajcmi.2021.25.

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Background: The growing spread of drug resistance in Helicobacter pylori has caused concern. Urease is one of the most important enzymes associated with H. pylori activity. Oxadiazoles have a wide range of inhibitory activities. The aim of this study was to investigate new oxadiazole compounds as urease inhibitors of H. pylori. Methods: The synthesized compounds were reused as ligands in the previous study, and the initial structure of the compounds was optimized by the Molecular Mechanics Models method. Then, the compounds were evaluated as inhibitors on the active site of the urease enzyme b

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47

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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48

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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49

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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50

Munukoti, Bhaskararao, and Venkateswara Rao Battula. "One-pot ultrasonication assisted synthesis of biologically active 1, 3, 4- oxadiazole derivatives catalyzed by TiO2 nanoparticles." Research Journal of Chemistry and Environment 26, no. 5 (2022): 168–76. http://dx.doi.org/10.25303/2605rjce168176.

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A novel approach was adopted in the one-pot synthesis of 2-phenyl-5-aryl substituted-1, 3, 4-oxadiazole derivatives through ultrasonication. Substituted carboxylic acids (1a-l) underwent condensation with benzohydrazide (13) in the presence of ortho- (benzotriazol-1-yl)-N, N, Nʹ, Nʹ-tetramethyluronium tetrafluoroborate (TBTU) to form diacylhydrazine derivatives (3a-l). In the next step, the derivatives 3a-l were subjected to cyclodehydration in the presence of titanium dioxide (TiO2) nanoparticles (NPs) in the presence of dichloromethane (DCM) solvent, at room temperature through which excelle

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