56352-92-2

Upstream product

• 614-18-6 3-pyridinecarboxylic acid ethyl ester 
• 553-53-7 Nicotinic acid hydrazide 
• 209797-67-1 ethyl p-methylbenzoateformylhydrazone 
• 99-94-5 p-Toluic acid 
• 56352-78-4 4-methylbenzoic acid(pyridine-3-carbonyl)hydrazide 

Downstream Products

• 1246493-40-2 3-(3-pyridyl)-5-(4-methylphenyl)-4-(N-(6-bromo-1,3-benzothiazol-2-yl)amino)-4H-1,2,4-triazole 
• 1246493-46-8 3-(3-pyridyl)-5-(4-methylphenyl)-4-(N-(4-nitro-1,3-benzothiazol-2-yl)amino)-4H-1,2,4-triazole 
• 1246493-47-9 3-(3-pyridyl)-5-(4-methylphenyl)-4-(N-(5,6-dichloro-1,3-benzothiazol-2-yl)amino)-4H-1,2,4-triazole 
• 1246493-42-4 3-(3-pyridyl)-5-(4-methylphenyl)-4-(N-(6-methyl-1,3-benzothiazol-2-yl)amino)-4H-1,2,4-triazole 
• 1246493-45-7 3-(3-pyridyl)-5-(4-methylphenyl)-4-(N-(4-methyl-1,3-benzothiazol-2-yl)amino)-4H-1,2,4-triazole 
• 1246493-43-5 3-(3-pyridyl)-5-(4-methylphenyl)-4-(N-(6-methoxy-1,3-benzothiazol-2-yl)amino)-4H-1,2,4-triazole 
• 1246493-41-3 3-(3-pyridyl)-5-(4-methylphenyl)-4-(N-(6-nitro-1,3-benzothiazol-2-yl)amino)-4H-1,2,4-triazole 
• 1246493-39-9 3-(3-pyridyl)-5-(4-methylphenyl)-4-(N-(6-fluoro-1,3-benzothiazol-2-yl)amino)-4H-1,2,4-triazole 
• 1246493-44-6 3-(3-pyridyl)-5-(4-methylphenyl)-4-(N-(6-chloro-1,3-benzothiazol-2-yl)amino)-4H-1,2,4-triazole 
• 1246493-48-0 3-(3-pyridyl)-5-(4-methylphenyl)-4-(N-(4-chloro-1,3-benzothiazol-2-yl)amino)-4H-1,2,4-triazole 

Relevant academic research and scientific papers

2,5-Disubstituted-1,3,4-oxadiazoles: Thymidine phosphorylase inhibitors

A series of 2,5-disubstituted-1,3,4-oxadiazoles (1-16) were synthesized via microwave irradiation and screened against thymidine phosphorylase enzyme. Four members of the series have demonstrated thymidine phosphorylase inhibitory activities with IC50 values between 37 and 320 μM. Pyridinyl-containing 1,3,4-oxadiazoles exhibited an enhanced inhibitory potential, while phenyl analogs did not show substantial inhibitory potential. Compound 9, a dipyridinyl residue having an IC50 value of 37 ± 0.76 μM was found to be the most potent in the series superior to standard inhibitor 7-deazaxanthine (IC50 = 39.28 ± 0.76 μM). Graphical abstract: [InlineMediaObject not available: see fulltext.]

Use of ester formylhydrazones for the synthesis of 1,2,4-triazole and 1,3,4-oxadiazole derivatives

A series of ester formylhydrazones were synthesised by the reaction of alkyl imidate hydrochlorides with ormylhydrazine. Treatment of the ester formylhydrazones with acetic acid hydrazide, isonicotinic acid hydrazide, nicotinicacid hydrazide, and 4-hydroxybenzhydrazide resulted in the formation of either 4-acylamino-4H-1,2,4-triazoles or 2,5-disubstituted 1,3,4-oxadiazoles. 3-Alkyl-4-amino-4,5-dihydro-1H-1,2,4-triazol-5-ones were synthesised by the reaction of the ester formylhydrazones with carbohydrazide. Some arylidenamino compounds were synthesized by the reaction of 4-amino-4,5-dihydro-1H-1,2,4- triazol-5-ones with several aldehydes. These compounds were characterised by elemental analyses, IR, 1H NMR, and UV spectral techniques.

Pharmacological evaluation and characterizations of newly synthesized 1,2,4-triazoles

The triazole analogs were obtained via. multistep synthesis sequence beginning with ethyl nicotinoate 3 which on treatment with hydrazine hydrate yields nicotinoyl hydrazide 4. Intermolecular cyclisation of 4 with 4-methylbenzoic acid in presence of phosphorous oxy chloride affords 2-(3-pyridyl)-5-(4-methylphenyl)-1,3,4-oxadiazole 5. Condensation of 5 with various substituted 2-hydrazino benzothiazole 2a-j results in 3-(3-pyridyl)-5-(4-methylphenyl)-4-(N-substituted-1,3-benzothiazol-2-amino) -4H-1,2,4-triazole 6a-j analogs. All the compounds have been characterized by elemental analysis, IR, 1H NMR, 13C NMR and mass spectral data. In vitro antitubercular activity was carried out against Mycobacterium tuberculosis H37Rv strain using Lowenstein-Jensen medium and antimicrobial activity against various bacteria and fungi using broth microdilution method. Compounds 2e, 6a, 6b, 6c, 6d, 6g, 6h and 6i emerged as promising antimicrobials. It was also observed that the promising antimicrobials have proved to be better antituberculars. Compound 6j showed better antitubercular activity compared to rifampicin. 3-(3-Pyridyl)-5-(4-methylphenyl) -4-(N-substituted-1,3-benzothiazol-2-amino)-4H-1,2,4-triazole 6a-j were synthesized and their antitubercular activity against H37Rv and antimicrobial activities have been tested.

HETEROCYCLIC COMPOUNDS AND THEIR METHODS OF USE

The invention relates to heterocyclic derivatives, compositions comprising such compounds, and methods of preventing or treating conditions and disorders using such compounds and compositions. The heterocyclic derivatives, more particularly can be substit

Synthesis and characterization of new blue-greenish electroluminescent materials based on 1,3,4-oxadiazole-triazolopyridinone hybrids

New functionalized oxadiazole-triazolopyridinone derivatives were synthesized via arcycloaddition. With the chromophores of triazolopyridinone, the photoluminescence spectra of these compounds in dichloromethane solution showed emission peaks between 430 and 520 nm. Following the spectroscopic studies, and the measurements of cyclic voltammogram, 1,3,4-oxadiazole- triazolopyridinone hybrids possess a great potential as highly efficient, blue-greenish, organic light-emitting devices materials.

Oxidative cyclization of aromatic aldehyde n-acylhydrazones by bis(trifluoroacetoxy)iodobenzene

Aromatic aldehyde N-acylhydrazones were oxidized into 2,5-disubstituted 1,3,4-oxadiazoles with bis(trifluoroacetoxy)iodobenzene in CHCl3 or DMSO at room temperature in good to excellent yields. Copyright Taylor & Francis Group, LLC.

Structure-activity relationships of tyrosinase inhibitory combinatorial library of 2,5-disubstituted-1,3,4-oxadiazole analogues

Here the tyrosinase inhibition studies of library of 2,5-disubstituted-1,3, 4-oxadiazoles have been reported and their structure-activity relationship (SAR) also have been discussed. The library of the oxadiazoles was synthesized under the microwave irradiation and was structures of these were characterized by different spectral techniques. From this study it could be concluded that for a better inhibition of tyrosinase, electronegative substitution is essential as most probably the active site of the enzyme contain some hydrophobic site and position is also very important for the inhibition purposes due to the conformational space. The electronegativity of the compounds is somewhat proportional to the inhibitory activity. The compound 3e (3′-[5-(4′- bromophenyl)-1,3,4-oxadiazol-2-yl]pyridine) exhibited most potent (IC 50 = 2.18 μM) inhibition against the enzyme tyrosinase which is more potent than the standard potent inhibitor l-mimosine (IC50 = 3.68 μM). This molecule can be the best candidate as a lead compound for further development of drug for the treatments of several skin disorders.