13059-77-3Relevant academic research and scientific papers
A Simple Isoniazid-Based N-Acylhydrazone Derivative as Potential Fluorogenic Probe for Zn2+ Ions
Santos, Daniela Corrêa,Maia, Paulo José Sousa,de Abreu Lopes Jr, Marcos Antonio,Forero, Josué Sebastián Bello,de Souza, Andréa Luzia Ferreira
, p. 175 - 184 (2021)
This study evaluated three isoniazid-based N-acylhydrazone derivatives (HL1, HL2, and HL3) varying their substituting groups (-H, -N(CH3)2, and -NO2) as potential chemosensors for Zn2+ ions. To this end, the absorption and emission properties of these derivatives were investigated in the presence of Zn2+ ions. Results point to the derivative HL2 as the best chemosensor for Zn2+ ions because of its comparatively higher sensitivity. The color of this derivative changed from colorless to strong yellow with zinc addition, as indicated by the shift in UV-vis spectrum. Moreover, HL2 was the only derivative to emit fluorescence in the presence of Zn2+ ions, attributable to PET inhibition and bond isomerization promoted by coordination with this metal. LOD, LOQ, and binding constant values for HL2 + Zn2+ were 0.43?μmol.l?1, 0.93?μmol.l?1, and 5.04 × 1012?l.mol?1, respectively. The fluorescence of HL2 with other metal ions (Fe3+, Mg2+, Na+, Cd2+, Cu2+, Co2+, Ni2+, Ca2+, and K+) was also investigated. Zn2+ yielded the best result without Cd2+ interferences. Job’s Plot showed that the stoichiometric ratio of the complex formed by HL2 and Zn2+ ions is 2:1 (ligand:metal). The strip test with adsorbed HL2 indicated fluorescence in the presence of zinc ions under 365?nm UV irradiation.
Two new 1D zigzag Hg(II) nanostructure coordination polymers: Sonochemical synthesis, thermal study, crystal structure and Hirshfeld surface analysis
Montazerozohori,Masoudiasl,Doert, Th.
, p. 207 - 217 (2016)
Reaction of mercury(II) chloride and bromide with a Schiff base ligand based on isonicotinohydrazide (L) yielded two new 1D zigzag coordination polymers; [Hg(μ-L)Cl2]n (1) and [Hg(μ-L)Br2]n (2). The Schiff base
Synthesis, characterization and antiamoebic activity of some hydrazone and azole derivatives bearing pyridyl moiety as a promising heterocyclic scaffold
Siddiqui, Shadab Miyan,Salahuddin, Attar,Azam, Amir
, p. 411 - 416 (2012)
In an effort to develop effective antiamoebic agents, some hydrazones and azoles containing pyridyl moiety were synthesized and screened for in vitro antiamoebic activity against HM1:IMSS strain of Entamoeba histolytica. Among all the compounds, only five compounds (1, 3, 5, 9 and 11) were found to be better inhibitors of growth of E. histolytica than the reference drug metronidazole. The cytotoxic studies of these compounds on human breast cancer MCF-7 cell line revealed that all the compounds were low-cytotoxic in the concentration range of 2.5-250 μM.
A new coordination polymer constructed from Pb(NO3)2 and a benzylideneisonicotinohydrazide derivative: Coordination-induced generation of a π-hole towards a tetrel-bonding stabilized structure
Mahmoudi, Ghodrat,Masoudiasl, Ardavan,Afkhami, Farhad Akbari,White, Jonathan M.,Zangrando, Ennio,Gurbanov, Atash V.,Frontera, Antonio,Safin, Damir A.
, (2021)
We report on a new Pb(II) coordination polymer [Pb(HL)(NO3)2]n (1), obtained from a direct reaction of Pb(NO3)2 with N'-4-(dimethylamino)benzylideneisonicotinohydrazide (HL). The coordination sphere a
Solvent-free and catalysis-free approach to the solid state in situ growth of crystalline isoniazid hydrazones
Trzesowska-Kruszynska, Agata
, p. 3892 - 3900 (2013)
The isonicotinoylhydrazones and their coordination compounds have antibacterial, antifungal, antitubercular, antitumor, and anticonvulsant activities. A typical method employed in the preparation of isonicotinoylhydrazones involves the usage of the volati
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
, (2020/04/15)
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.
Design and Synthesis of 5-Oxoimidazolidine Derivatives in Search of Potent Antitubercular and Antifungal agents
Singirisetty, Triveni,Chilamakuru, Naresh Babu,Peraman, Ramalingam,Mallela, Vijaya Jyothi,Sana, Maheswari P.,Begum, Inthiyaz
, p. 441 - 451 (2021/02/02)
5-Oxoimidazolidines are significant outfits because of their impending biological activity and also because of their resourcefulness as synthons in organic revolutions. The designed library was docked against the crystal structure of Mycobacterium tuberculosis enoyl reductase (2B35) and crystal structure of flavohemoglobin (3OZU) to know the best fit molecule. The ADMET parameters revealed that the compounds have synthetic acceptability and leadlikeness. Accordingly, the selected 5-oxoimidazolidines (S1-8 and A1-8) were synthesized from carbohydrazides (1a-h) and characterized by spectral data. Further, these compounds were screened against M. tuberculosis H37RV by microplate Alamar Blue assay method. The compound S3 showed minimum inhibitory concentration at 6.25 μg/mL, while the antifungal screening demonstrated S1 as a promising lead with the corresponding zone of inhibitions of 22 mm and 18 mm against Aspergillus niger and Candida albicans.
Organoboron compound based on acyl hydrazone ligand and preparation method and application thereof
-
Paragraph 0086; 0090-0092, (2019/12/08)
The invention relates to an organoboron compound based on an acyl hydrazone ligand and a preparation method and an application thereof. A series of organoboron fluorescent compounds based on acyl hydrazone ligands synthesized by the invention are easy to
Antimicrobial activities of synthetic arylidine nicotinic and isonicotinic hydrazones
Hayat, Muhammad,Khan, Khalid Mohammed,Saeed, Sumayya,Salar, Uzma,Khan, Momin,Baig, Taimoor,Ahmad, Aqeel,Parveen, Shahnaz,Taha, Muhammad
, p. 1057 - 1067 (2018/10/31)
Background: Despite availability of variety of antibacterial agents, re-emergance of pathogenic bacteria is still a serious medical concern. Identification of new, safer, and selective antibacterial agents is the key interest in the medicinal chemistry research. Methods: A library of synthetic arylidene nicotinic and isonicotinic hydrazones (1-63) were investigated for antimicrobial activities. Results: A number of derivatives showed significant to moderate antimicrobial activities against Gram positive and Gram negative bacterial cultures. Few compounds also showed antifungal activity against fungal cultures. Minimum Inhibitory Concentration (MIC) was calculated for the most active compounds 1, 7, 11, 19, 34, 46, 50, 51, and 55 against gram positive and gram negative cultures. Conclusion: Newly identified compounds may serve as lead for future research in order to get the more powerful antibacterial agents.
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
