533-02-8Relevant academic research and scientific papers
Synthesis, inhibition of mycobacterium tuberculosis enoyl-acyl carrier protein reductase and antimycobacterial activity of novel pentacyanoferrate(II)-isonicotinoylhydrazones
Gazzi, Thais P.,Rotta, Mariane,Villela, Anne D.,Rodrigues, Valn's,Martinelli, Leonardo K.B.,Sales, Francisco Adilson M.,Silva De Sousa, Eduardo Henrique,Campos, Maria Martha,Basso, Luiz Augusto,Santos, Diógenes S.,Machado, Pablo
, p. 2028 - 2037 (2017/09/01)
Tuberculosis remains among the top causes of death triggered by a single pathogen. Herein, a greener synthetic approach for isonicotinoylhydrazones is described using ultrasound energy. These compounds were used as starting materials for synthesizing pent
Xanthine oxidase inhibitory activity of nicotino/isonicotinohydrazides: A systematic approach from in vitro, in silico to in vivo studies
Zafar, Humaira,Hayat, Muhammad,Saied, Sumayya,Khan, Momin,Salar, Uzma,Malik, Rizwana,Choudhary, M. Iqbal,Khan, Khalid Mohammed
, p. 2351 - 2371 (2017/04/03)
Change in life style and eating habits has led to an increased prevalence of hyperuricemia worldwide. The role of hyperuricemia is no more restricted to gout, but it has a central role in progression of CVD, hypertension, metabolic syndrome, and arthritis
MFA zeotype catalyst: A greener approach for the synthesis of INH azomethine scaffolds
Raghuvanshi, Devendra S.,Mahulikar, Pramod P.,Meshram, Jyotsna S.
, p. 48071 - 48078 (2015/06/16)
Herein, we are reporting the green and efficient synthesis of some pharmacologically important azomethine derivatives of isoniazide (INH) using Modified Fly Ash (MFA) as an excellent zeotic solid acid catalyst. The catalyst, by virtue of its terminal hydr
Acylhydrazones as Widely Tunable Photoswitches
Van Dijken, Derk Jan,Kova?í?ek, Petr,Ihrig, Svante P.,Hecht, Stefan
supporting information, p. 14982 - 14991 (2015/12/08)
Molecular photoswitches have attracted much attention in biological and materials contexts. Despite the fact that existing classes of these highly interesting functional molecules have been heavily investigated and optimized, distinct obstacles and inherent limitations remain. Considerable synthetic efforts and complex structure-property relationships render the development and exploitation of new photoswitch families difficult. Here, we focus our attention on acylhydrazones: a novel, yet underexploited class of photochromic molecules based on the imine structural motif. We optimized the synthesis of these potent photoswitches and prepared a library of over 40 compounds, bearing different substituents in all four crucial positions of the backbone fragment, and conducted a systematic study of their photochromic properties as a function of structural variation. This modular family of organic photoswitches offers a unique combination of properties and the compounds are easily prepared on large scales within hours, through an atom-economic synthesis, from commercially available starting materials. During our thorough spectroscopic investigations, we identified photoswitches covering a wide range of thermal half-lives of their (Z)-isomers, from short-lived T-type to thermally stable P-type derivatives. By proper substitution, excellent band separation between the absorbance maxima of (E)- and (Z)-isomers in the UV or visible region could be achieved. Our library furthermore includes notable examples of rare negative photochromic systems, and we show that acylhydrazones are highly fatigue resistant and exhibit good quantum yields.
Structure-based optimization of oxadiazole-based GSK-3 inhibitors
Lo Monte, Fabio,Kramer, Thomas,Gu, Jiamin,Brodrecht, Martin,Pilakowski, Johannes,Fuertes, Ana,Dominguez, Juan Manuel,Plotkin, Batya,Eldar-Finkelman, Hagit,Schmidt, Boris
, p. 26 - 40 (2013/04/23)
Inhibition of glycogen synthase kinase-3 (GSK-3) induces neuroprotective effects, e.g. decreases β-amyloid production and reduces tau hyperphosphorylation, which are both associated with Alzheimer's disease (AD). The two isoforms of GSK-3 in mammalians are GSK-3α and β, which share 98% homology in their catalytic domains. We investigated GSK-3 inhibitors based on 2 different scaffolds in order to elucidate the demands of the ATP-binding pocket [1]. Particularly, the oxadiazole scaffold provided potent and selective GSK-3 inhibitors. For example, the most potent inhibitor of the present series, the acetamide 26d, is characterized by an IC50 of 2 nM for GSK-3α and 17 nM for GSK-3β. In addition, the benzodioxane 8g showed up to 27-fold selectivity for GSK-3α over GSK-3β, with an IC 50 of 35 nM for GSK-3α. Two GSK-3 inhibitors were further profiled for efficacy and toxicity in the wild-type (wt) zebrafish embryo assay to evaluate simultaneously permeability and safety.
Synthesis and characterization of (E)-N′-(substituted benzylidene)isonicotinohydrazide derivatives as potent antimicrobial and hydrogen peroxide scavenging agents
Malhotra, Manav,Sharma, Gaurav,Deep, Aakash
experimental part, p. 637 - 644 (2012/08/29)
A series of (E)-N′-(substituted benzylidene)isonicotinohydrazide derivatives were synthesized by coupling isoniazid with differently substituted aldehydes and benzophenones in the presence of absolute ethanol along with catalytic amount of glacial acetic
Synthesis, characterization and pharmacological evaluation of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives as potent anticonvulsant agents
Malhotra, Manav,Monga, Vikramdeep,Sharma, Sagun,Jain, Jainendra,Samad, Abdul,Stables, James,Deep, Aakash
, p. 2145 - 2152 (2012/11/07)
A series of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives were synthesized by coupling it with different substituted aldehydes, acetophenone, and benzophenones in presence of absolute ethanol along with catalytic amount of glacial aceti
Synthesis and anti-mycobacterial activity of (E)-N′-(monosubstituted-benzylidene)isonicotinohydrazide derivatives
Lourenco, Maria Cristina da Silva,Ferreira, Marcelle de Lima,de Souza, Marcus Vinicius Nora,Peralta, Monica Amado,Vasconcelos, Thatyana Rocha Alves,Henriques, Maria das Gracas M.O.
, p. 1344 - 1347 (2008/09/21)
A series of 22 (E)-N′-(monosubstituted-benzylidene)isonicotinohydrazide derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv using Alamar Blue susceptibility test and
Modifications of boronic ester pro-chelators triggered by hydrogen peroxide tune reactivity to inhibit metal-promoted oxidative stress
Charkoudian, Louise K.,Pham, David M.,Kwon, Ashley M.,Vangeloff, Abbey D.,Franz, Katherine J.
, p. 5031 - 5042 (2008/03/13)
Several new analogs of salicylaldehyde isonicotinoyl hydrazone (SIH) and salicylaldehyde benzoyl hydrazone (SBH) that contain an aryl boronic ester (BSIH, BSBH) or acid (BASIH) in place of an aryl hydroxide have been synthesized and characterized as maske
