382178-47-4Relevant academic research and scientific papers
Synthesis of some 2,3-dihydro-1,3,4-oxadiazoles and 4,5-dihydro-1,2,4-triazoles as anticancer agents
Abdullah, Jalal H.,Yahya, Tawfeek A.
, p. 92 - 99 (2020/09/02)
Objective: The main objective of this work was to synthesize and evaluate the novel 2,3-dihydro-1,3,4-oxadiazole and 4,5-dihydro-1,2,4-triazole derivatives for cytotoxic activities. Methods: The 2,3-dihydro-1,3,4-oxadiazole derivatives 4a-h were synthesized by cyclization of N'-(substituted-benzylidene) isonicotinohydrazide 3a-e in refluxing acetic anhydride. The 2,3-dihydro-1,3,4-oxadiazole derivatives 4a-h were converted into the corresponding 4,5-dihydro-1,2,4-triazoles 5a-h using ammonia. All the synthesized compounds were identified, depending on the physical and spectral data. Title compounds were assessed for their cytotoxic activity against human cancer cell line (MCF-7) by using Sulforhodamine B (SRB) colorimetric assay. Results: All the synthesized compounds showed characteristic peaks in FTIR, 1HNMR and Mass spectral analysis. The results of the in vitro cytotoxic activity revealed that the compound 4c exhibited equipotent cytotoxic activity with an IC50 value of 8.04 μM when compared with that of standard drug doxorubicin (IC50= 8.02 μM). The reminder compounds have shown good to moderate cytotoxic activities when compared with that of a reference standard. Conclusion: We synthesized a series of title compounds in quantitative yields. Most derivatives showed moderate to good cytotoxic activity.
Endothelium dependent and independent mechanisms of vasorelaxant activity of synthesized 2,5-disubstituted-1,3,4-oxadiazole derivatives in rat thoracic aorta-ex vivo and molecular docking studies
Attari, Zenab,Mudgal, Jayesh,Nayak, Pawan G.,Krishnadas, Nandakumar,Rajappan, Revathi,Gopalan Kutty
, p. 441 - 450 (2016/05/19)
Background: Vasoconstriction is a major pathological feature of cardiovascular diseases involving endothelium dependent and independent mechanisms. Oxadiazole moiety appeared to be effective in various pathologies. Objective: The aim of the study was to s
Synthesis and testing of 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4- oxadiazole derivatives for antifungal activity against selected Candida species
De Oliveira, Cledualdo S.,Lira, Bruno F.,Barbosa-Filho, Jose? M.,Lorenzo, Jorge G. F.,De Menezes, Camilla P.,Dos Santos, Jessyca M. C. G.,De Lima, Edeltrudes O.,De Athayde-Filho, Petro?nio F.
, p. 115 - 120 (2013/04/24)
A series of 21 1,3,4-oxadiazoline derivatives was synthesized by cyclization of N-acylhydrazones with acetic anhydride and evaluated for their in vitro antifungal activity against six Candida strains: Candida albicans (ATCC 90028 and LM V-42), C. krusei (ATCC 6258 and LM 12 C) and C. tropicalis (ATCC 13803 and LM 14). The Candida strains were found to be sensitive to some of the compounds, which inhibited the growth by 50-90percent, with minimum inhibitory concentration (MIC) in the range of 64-512 μg mL-1. The compounds' structures were fully confirmed and characterized by Fourier transform infrared spectroscopy (FTIR), 1H and 13C nuclear magnetic resonance (NMR) and mass spectrometry (MS).
Thiazolidin-4-one, azetidin-2-one and 1,3,4-oxadiazole derivatives of isonicotinic acid hydrazide: Synthesis and their biological evaluation
Gilani, Sadaf J.,Khan, Suroor A.,Alam, Ozair,Singh, Vijender,Arora, Alka
, p. 1057 - 1067 (2012/02/05)
A series of thiazolidin-4-one (2a-h; 3a-h), azetidin-2-one (4a-h) and 1,3,4-oxadiazole (5a-h) derivatives of isoninicotinic acid hydrazide (INH) were synthesized in order to obtain new compounds with potential anti-inflammatory, analgesic, ulcerogenic and
3-Acetyl-2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoles: A new scaffold for the selective inhibition of monoamine oxidase B
MacCioni, Elias,Alcaro, Stefano,Cirilli, Roberto,Vigo, Sara,Cardia, Maria Cristina,Sanna, Maria Luisa,Meleddu, Rita,Yanez, Matilde,Costa, Giosuè,Casu, Laura,Matyus, Peter,Distinto, Simona
experimental part, p. 6394 - 6398 (2011/11/06)
3-Acetyl-2,5-diaryl-2,3-dihydro-1,3,4-oxadiazoles were designed, synthesized, and tested as inhibitors against human monoamine oxidase (MAO) A and B isoforms. Several compounds, obtained as racemates, were identified as selective MAO-B inhibitors. The enantiomers of some derivatives were separated by enantioselective HPLC and tested. The R-enantiomers always showed the highest activity. Docking study and molecular dynamic simulations demonstrated the putative binding mode. We conclude that these 1,3,4-oxadiazoles derivatives are promising reversible and selective MAO-B inhibitors.
