86189-87-9Relevant academic research and scientific papers
Acylhydrazones as isoniazid derivatives with multi-target profiles for the treatment of Alzheimer's disease: Radical scavenging, myeloperoxidase/acetylcholinesterase inhibition and biometal chelation
Henriques, Ruan Roberto,Junior, Marcos Antonio de Abreu Lopes,Nogueira, Thayssa Lisboa do Couto,Romeiro, Nelilma Correia,Silva, Leandro Louback da,Farias, André Borges,Quimas, Jo?o Victor Fernandes,Santos, Daniela Corrêa,Souza, Andréa Luzia Ferreira de
, (2020)
Acylhydrazones 1a-o, derived from isoniazid, were synthesized and evaluated for Myeloperoxidase (MPO) and Acetylcholinesterase (AChE) inhibition, as well as their antioxidant and metal chelating activities, with the purpose of investigating potential multi-target profiles for the treatment of Alzheimer's disease. Synthesized compounds were tested using the 2,2-diphenyl-2-picrylhydrazyl (DPPH) method and 1i, 1j and 1 m showed radical scavenging ability. Compounds 1b, 1 h, 1i, 1 m and 1o inhibited MPO activity (10 μM) at 96.1 ± 5.5%, 90 ± 2.1%, 100.3 ± 1.7%, 80.1 ± 9.4% and 82.2 ± 10.6%, respectively, and only compound 1 m was able to inhibit 54.2 ± 1.7% of AChE activity (100 μM). Docking studies of the most potent compound 1 m were carried out, and the computational results provided the theoretical basis of enzyme inhibition. Furthermore, compound 1 m was able to form complexes with Fe2+ and Zn2+ ions in a 2:1 ligand:metal ratio according to the Job Plot method.
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
Design, synthesis, characterization, cytotoxic and structure activity relationships of novel Ru(II) complexes
Thota, Sreekanth,Vallala, Srujana,Yerra, Rajeshwar,Barreiro, Eliezer J.
, p. 721 - 726 (2015/07/27)
Abstract Platinum containing compounds have shown antineoplastic potential, but their clinical applications have been limited by high toxicity. Ruthenium containing complexes have long been known to be well suited for biological applications, and have lon
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).
Synthesis and biological screening of some pyridine derivatives as anti-malarial agents
Bekhit, Adnan A.,Hymete, Ariaya,Damtew, Ashenafi,Mohamed, Abdel Maaboud I.,Bekhit, Alaa El-Din A.
experimental part, p. 69 - 77 (2012/04/05)
Two series of pyridine derivatives were synthesised and evaluated for their in vivo anti-malarial activity against Plasmodium berghei. The anti-malarial activity was determined in vivo by applying 4-day standard suppressive test using chloroquine (CQ)-sen
Synthesis and biological screening of Some 1,3,4-oxadiazoles
Ishwar Bhat,Revanasiddappa,Prems, Jisha,Mumtaz Mohammed Hussain
, p. 183 - 184 (2013/09/24)
Treatment of Schiff bases with yellow mercuric oxide and iodine in DMF medium yields the title compounds 1,3,4-oxadiazoles (4a-j). The structures of the newly synthesized compounds were assigned on the basis of IR, 1H NMR, Mass spectral data and elemental analysis. All the new compounds were evaluated for their in vitro antibacterial and antifungal activity. Some of the new compounds showed good activity against some bacteria when compared with the standard drug.
Halogenated isoniazid derivatives as possible antitubercular and antineoplastic agents. Note 1
Vigorita,Basile,Zappala,Gabrielli,Pizzimenti
, p. 893 - 906 (2007/10/02)
Halogenated arylhydrazones, 2-aryl-4-thiazolidinones and their 1,1-dioxides containing isoniazid (INI) moieties were prepared and explored for antimicrobial (against bacteria, Candida and mycobacteria) and antitumor activities. None of the tested compound
