15017-32-0Relevant academic research and scientific papers
Synthesis, structural characterization, and molecular docking studies of bioactive bismuth(III) complexes with substituted hydrazones
Abbas, Sumaira,Imtiaz-ud-Din,Mehmood, Mehwish,Rauf, M. Khawar,Azam, S. Sikander,Haq, Ihsan-ul,Tahir, M. Nawaz,Parvaiz, Nousheen
, (2021)
Eight new bismuth(III) complexes (1-8) of substituted hydrazones having general formula; [Bi(RCONHNCHC5H4N)Clx] and [Bi(RCONHNCHC9H6N)Clx], where R = C10H7O (1, and 8)
Thermodynamics of the complexation of N-(pyridin-2-ylmethylene) isonicotinohydrazide with lighter lanthanides
Yumnam, Sharmeli,Rajkumari, Lonibala
, p. 28 - 34 (2009)
N-(Pyridin-2-ylmethylene)isonicotinohydrazide, pmINH, has been synthesized and characterized on the basis of elemental and spectral data. The protonation constants of pmINH and the stability constants of the base with trivalent La, Pr, Nd, Sm, Eu, and Gd at constant ionic strength (I, mol·-dm -3 = 0.05 M NaClO4) and at different temperatures, T = (293, 303, and 313) K, were determined potentiometrically in water-dioxane (30 %) medium. The ligand forms only 1:1 complexes with the lanthanides. Both protonation and complexation reactions are found to be exothermic in nature. The trend in the formation constants follows the order: La3+ 3+ 3+ 3+ 3+ 3+ and shows a break at gadolinium. The thermodynamic parameters associated with the complexation reactions were also calculated. The values of AG, AH, and AS are negative for all the systems and suggest that all reactions are enthalpy driven. The thermodynamic parameters of the complexation are correlated with the reciprocal ionic radii of the metal ions. Raw and normalized isothermal calorimetric data for the titrations of Gd 3+-pmINH solutions at 303 K show that the reaction was exothermic and metal-ligand stoichiometry to be 1:1.
Syntheses, characterization and crystal structures of potassium and barium complexes of a Schiff base ligand with different anions
Parmar, Bhavesh,Bisht, Kamal Kumar,Maiti, Pratyush,Paul, Parimal,Suresh, Eringathodi
, p. 1373 - 1384 (2014)
New pseudopolymorph of a O,N,N'-donor hydrazone ligand, 2-pyridylcarboxaldehyde isonicotinoylhydrazone (L) and its discrete complexes with K+ and Ba2+ have been reported. L forms isostructural dinuclear complexes with K+ when bromide and iodide were employed as counter anions. However, a monomeric complex in the case of Ba2+ with existence of coordinated as well as lattice perchlorate counter anions was observed. All compounds were characterized by single crystal X-ray analysis and other physicochemical techniques. Structural analysis and spectral features of all compounds are described in detail.
N-acylhydrazones confer inhibitory efficacy against New Delhi metallo-β-lactamase-1
Gao, Han,Li, Jia-Qi,Kang, Peng-Wei,Chigan, Jia-Zhu,Wang, Huan,Liu, Lu,Xu, Yin-Sui,Zhai, Le,Yang, Ke-Wu
, (2021/07/07)
The expression of β-lactamases, especially metallo-β-lactamases (MβLs) in bacteria is one of the main causes of drug resistance. In this work, an effective N-acylhydrazone scaffold as MβL inhibitor was constructed and characterized. The biological activity assays indicated that the synthesized N-acylhydrazones 1–11 preferentially inhibited MβL NDM-1, and 1 was found to be the most effective inhibitor with an IC50 of 1.2 μM. Analysis of IC50 data revealed a structure–activity relationship, which is that the pyridine and hydroxylbenzene substituents at 2-position improved inhibition of the compounds on NDM-1. ITC and enzyme kinetics assays suggested that it reversibly and competitively inhibited NDM-1 (Ki = 0.29 ± 0.05 μM). The synthesized N-acylhydrazones showed synergistic antibacterial activities with meropenem, reduced 4–16-fold MIC of meropenem on NDM-1- producing E. coli BL21 (DE3), while 1 restored 4-fold activity of meropenem on K. pneumonia expressing NDM-1 (NDM-K. pneumoniae). The mice experiments suggested that 1 combined meropenem to fight against NDM-K. pneumoniae infection in the spleen and liver. Cytotoxicity assays showed that 1 and 2 have low cytotoxicity. This study offered a new framework for the development of NDM-1 inhibitors.
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.
Preparation and acetylcholinesterase inhibitory activities of pyridine-based 1,3,4-oxadiazole derivatives
Chen, Yafang,Huang, Ling,Yang, Wude,Yu, Xiang,Zhou, Xingji
, p. 1163 - 1171 (2020/09/18)
Fourteen pyridine-based 1,3,4-oxadiazole derivatives were synthesized from pyridine-2-carboxaldehyde via iodine-mediated oxidative cyclisation with substituted hydrazide by using the impregnation method. Their structures were confirmed by melting point,
Synthesis, crystal structures, characterization and catalytic property of manganese(II) complexes derived from hydrazone ligands
Tan, Yao
, p. 1233 - 1238 (2021/06/07)
A new bromido-coordinated mononuclear manganese(II) complex [MnL1Br2(OH2)] (1), and a new nitrato-coordinated mononuclear manganese(II) complex [Mn(L2)2(ONO2)(OH2)]NO3
Biological properties of heterocyclic pyridinylimines and pyridinylhydrazones
Martins, Francislene J.,Lima, Rebeca Ml,Dos Santos, Juliana Alves,De Almeida Machado, Patricia,Coimbra, Elaine Soares,Da Silva, Adilson David,Raposo, Ndia Rezende Barbosa
, p. 107 - 114 (2015/12/01)
This work describes the synthesis and biological properties of a series of 2- and 4-pyridinylimines and pyridinylhydrazones. All compounds were evaluated in vitro against two species of Leishmania. The antioxidant activity and the toxic effect against mur
Biological properties of heterocyclic pyridinylimines and pyridinylhydrazones
Martins, Francislene J.,Lima, Rebeca Mól,Dos Santos, Juliana Alves,De Almeida Machado, Patrícia,Coimbra, Elaine Soares,Da Silva, Adilson David,Raposo, Nádia Rezende Barbosa
, p. 107 - 114 (2015/11/17)
This work describes the synthesis and biological properties of a series of 2- and 4- pyridinylimines and pyridinylhydrazones. All compounds were evaluated in vitro against two species of Leishmania. The antioxidant activity and the toxic effect against mu
Synthesis, structural diversity and mimic superoxide dismutase of Mn(II) complexes derived from N, O-donor schiff bases
Qin, Jie,Yin, Qiang,Zhao, Shan-Shan,Wang, Jun-Zheng,Qian, Shao-Song
, p. 55 - 61 (2016/03/19)
Two new potentially tetradentate Schiff base ligands N'-(pyridin-2-ylmethylene)nicotinohydrazide (L1), and N'-(pyridin-2-ylmethylene)isonicotinohydrazide (L2) were synthesized. Reactions of hydrazone ligands L1 and L2 with Mn(NO3)2 afford two mononuclear Mn(II) complexes, [Mn(L1)(NO3)(H2O)2]NO3 (1) and [Mn(L2)2 (NO3)(H2O)]NO3 (2). For complexes 1 and 2, L1 and L2 act as pincer-like tridentate or bidentate ligands, respectively. The Mn(II) ions in the two compounds are both in hepta-coordinated environment, while the two molecules display diverse solid-state supramolecular structures because of the different orientation of Npyridine and hydrogen bonding patterns of nitrate anions. Complex 1 features 2D supramolecular sheet, while complex 2 has double-chain supramolecular structure. Both of the complexes exhibit moderate superoxide dismutase (SOD) mimetic activity.
