893-42-5

Upstream product

• 54-85-3 isoniazid 
• 123-11-5 4-methoxy-benzaldehyde 
• 2459-09-8 4-pyridinecarboxylic acid, methyl ester 
• 55-22-1 pyridine-4-carboxylic acid 

Downstream Products

• 382178-48-5 2-(4-methoxyphenyl)-3-acetyl-5-(pyridin-4-yl)-2,3-dihydro-1,3,4-oxadiazole 
• 79844-16-9 N-[2-(4-methoxyphenyl)-4-oxo-1,3-thiazolidin-3-yl]pyridine-4-carboxamide 
• 1152134-80-9 N-[3-Chloro-2-(4-methoxyphenyl)-4-oxoazetidin-1-yl]pyridine-4-carboxamide 
• 100714-58-7 N'-(4-methoxybenzyl)isonicotinohydrazide 

Relevant academic research and scientific papers

p-Methoxybenzaldehyde isonicotinoylhydrazone monohydrate

X-ray analysis reveals that the title compound, C14H13N3O2·H2O, is in keto tautomeric form and the configuration at the azomethine C=N double bond is E. The pyridine plane makes a dihedral angle of 39

N-acylhydrazones confer inhibitory efficacy against New Delhi metallo-β-lactamase-1

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.

Synthesis, inhibition of mycobacterium tuberculosis enoyl-acyl carrier protein reductase and antimycobacterial activity of novel pentacyanoferrate(II)-isonicotinoylhydrazones

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

Spectroscopic, molecular docking and structural activity studies of (E)-N′-(substituted benzylidene/methylene) isonicotinohydrazide derivatives for DNA binding and their biological screening

Acid catalyzed condensation of isoniazid with a number of suitably substituted aromatic and heterocyclic aldehydes was carried out in dry ethanol to afford the title (E)-N′-(substituted benzylidene/methylene) isonicotinohydrazides (SF 1 – SF 4) in good yi

Isonicotinohydrazones as inhibitors of alkaline phosphatase and ecto-5′-nucleotidase

A series of isonicotinohydrazide derivatives was synthesized and tested against recombinant human and rat ecto-5′-nucleotidases (h-e5′NT and r-e5′NT) and alkaline phosphatase isozymes including both bovine tissue-non-specific alkaline phosphatase (b-TNAP)

Structure-based optimization of oxadiazole-based GSK-3 inhibitors

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, characterization and pharmacological evaluation of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives as potent anticonvulsant agents

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

Thiazolidin-4-one, azetidin-2-one and 1,3,4-oxadiazole derivatives of isonicotinic acid hydrazide: Synthesis and their biological evaluation

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

Synthesis, characterization of (E)-N'-(substituted-benzylidene) isonicotinohydrazide derivatives as potent antitubercular agents

A series of 19 isonicotinic acid hydrazide derivatives has been synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv using alamar blue susceptibility test. The synthesized comp

Synthesis and anti-mycobacterial activity of (E)-N′-(monosubstituted-benzylidene)isonicotinohydrazide derivatives

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