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Upstream product

• 55-22-1 pyridine-4-carboxylic acid 
• 1570-45-2 isonicotinic acid ethylester 
• 14389-12-9 5-(4-pyridyl)tetrazole 
• 100-07-2 4-methoxy-benzoyl chloride 
• 100-09-4 4-methoxybenzoic acid 
• 54-85-3 isoniazid 
• 123-11-5 4-methoxy-benzaldehyde 
• 151427-25-7 N-isonicotinoyl-N'-(4-methoxybenzoyl)hydrazine 

Relevant academic research and scientific papers

Synthesis of Pyridine Clubbed 2,5-Disubstituted-1,3,4-Oxadiazole Derivatives Shows Potent Antimicrobial Activity

In the present study, a series of 2,5-disubstituted-1,3,4 oxadiazole analogues retaining pyridine moiety were synthesized (4a-j) by reacting various substituted aromatic acids and isonicotinohydrazide by using POCl3 as a cycling agent. The structure elucidation of all the synthesized compounds was done by chromatographic data and spectral data analysis. The synthesized compounds were evaluated for their in-vitro antimicrobial activity against various strains of ESKAPE pathogens. Antibacterial activity was performed against Bacillus subtilis, Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa, while antifungal activity was assayed against Candida albicans and Aspergillus spp. The result of in-vitro antimicrobial studies of all the synthesized compounds revealed that compound 4d and 4f exhibited promising activity against selected microbial strains equally compared to Cefixime and Econazole used as reference drugs.

Cytotoxicity of η6-areneruthenium-based molecules to glioblastoma cells and their recognition by multidrug ABC transporters

A new series of amphiphilic η6-areneruthenium(II) compounds containing phenylazo ligands (group I: compounds 1a, 1b, 2a and 2b) and phenyloxadiazole ligands (group II: compounds 3a, 3b, 4a and 4b) were synthesized and characterized for their anti-glioblastoma activity. The effects of the amphiphilic η6-areneruthenium(II) complexes on the viability of three human glioblastoma cell lines, U251, U87MG and T98G, were evaluated. The azo-derivative ruthenium complexes (group I) showed high cytotoxicity to all cell lines, whilst most oxadiazole-derivative complexes (group II) were less cytotoxic, except for compound 4a. The cationic complexes 2a, 2b and 4b were more cytotoxic than the neutral complexes. Compounds 2a and 2b caused a significant reduction in the percentage of cells in the G0/G1 phase, with concomitant increases in the G2/M phase and fragmented DNA in the T98G cell line. The η6-areneruthenium(II) compounds were also tested in cell lines that overexpress the multidrug ABC transporters P-gp, MRP1 and ABCG2. Compounds 2b and 4a were substrates for the P-gp protein, with resistance indexes of 8.6 and 1.9, respectively. Compound 2b was also a substrate for ABCG2 and MRP1 proteins, with lower resistance indexes (1.8 and 1.6, respectively). The contribution of multidrug ABC transporters to the cytotoxicity of compound 2b in T98G cells was evidenced, since verapamil (a characteristic inhibitor of MRP1) increased the cytotoxicity of compound 2b at concentrations up to 20 μmol L?1, whilst GF120918 and Ko143 (specific inhibitors of P-gp and ABCG2, respectively) had no significant effect. In addition, we showed that compound 2b interacts with glutathione (GSH), which could explain its cellular efflux by MRP1. Our results showed that the amphiphilic η6-areneruthenium(II) complexes are promising anti-glioblastoma compounds, especially compound 2b, which was cytotoxic for all three cell lines, although it is transported by the three main multidrug ABC transporters.

Synthesis and biological screening of Some 1,3,4-oxadiazoles

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.

Convenient preparation of unsymmetrical 2,5-disubstituted 1,3,4-oxadiazoles promoted by Dess-Martin reagent

2,5-Disubstituted 1,3,4-oxadiazoles have been conveniently prepared by oxidative cyclization of N-acyl-N′-aryliden-hydrazines promoted by an excess of Dess-Martin periodinane under mild conditions (23 examples, up to 92% isolated yields).

A facile procedure for the one-pot synthesis of unsymmetrical 2,5-disubstituted 1,3,4-oxadiazoles

Unsymmetrically 2,5-disubstituted 1,3,4-oxadiazoles were efficiently synthesized from the cyclization-oxidation reaction of acyl hydrazones. Also, the synthesis of the title compounds was achieved by the condensation of acyl hydrazides and aromatic aldehydes in the presence of ceric ammonium nitrate in dichloromethane.

Iodobenzene diacetate mediated solid-state synthesis of heterocyclyl-1,3,4-oxadiazoles

A simple and efficient method has been developed for the oxidation of various heterocyclyl acylhydrazones 3 with iodobenzene diacetate (IBD) to heterocyclyl-1,3,4-oxadiazoles 4 in solid state. The reaction took place at room temperature within few minutes. The products were isolated by simple aqueous work-up in good yields.

Synthesis and biological activity of some isoniazid based 1,3,4-oxadiazole derivatives

1,3,4-Oxadiazole and isoniazid moieties are important because of their versatile biological actions. In the present studies, the oxadiazole system has been built with the isoniazid moiety and a few compounds in this series have been synthesised and their

An expeditious and convenient one pot synthesis of 2,5-disubstituted-1,3,4-oxadiazoles

A convenient, one pot procedure is reported for the synthesis of a variety of 2,5-disubstituted-1,3,4-oxadiazoles by condensing monoarylhydrazides with acid chlorides in HMPA solvent under the microwave heating. The yields are good to excellent, the process is rapid and does not need any added acid catalyst or dehydrating reagent.

Syntheses and Photophysical Properties of Some 5(2)-Aryl-2(5)-(4-pyridyl)oxazoles and Related Oxadiazoles and Furans

A number of 5-aryl-2-(4-pyridyl)oxazoles, a 2-aryl-5-(4-pyridyl)oxazole, the related oxadiazole and furan, several 2-(4-pyridyl)cycloalkanooxazoles, and many of their quaternary salts were prepared.No single standard synthesis was effective for preparation of more than a few of the 25 free bases described; methods often unique to a base were employed.Minor variations in structure sometimes produced large differences in absorption and emission wavelengths, as well as in the magnitude of the extinction coefficient.The salts are of interest as laser dyes, scintillation fluors, biological stains, and shifters for luminescent solar concentrators.