114659-72-2

Upstream product

• 553-53-7 Nicotinic acid hydrazide 
• 552-89-6 2-nitro-benzaldehyde 
• 10400-19-8 3-pyridinecarbonyl chloride 
• 614-18-6 3-pyridinecarboxylic acid ethyl ester 
• 59-67-6 nicotinic acid 

Downstream Products

• 1263151-26-3 1-(2-(2-nitrophenyl)-5-(pyridin-3-yl)-1,3,4-oxadiazole-3(2H)-yl) ethanone 

Relevant academic research and scientific papers

Investigation of nicotinamide and isonicotinamide derivatives: A quantitative and qualitative structural analysis

An anhydrous nature of benzylidene derivatives of nicotin and isonicotinamides crystal structures is determined and studied for their weak intermolecular interactions. The molecular structure is non-planar in general with the pyridine ring twisted with re

Synthesis and pharmacological evaluation of pyridinyl-1,3,4-oxadiazolyl-ethanone derivatives as antimicrobial, antifungal and antitubercular agents

Abstract: Nicotinic acid was converted into different substituted acetylated nicotinic acid derivatives by sequential transformation involving formation of hydrazide, Schiff’s base and finally acylated oxadiazole derivatives. The synthesized compounds were characterized by spectroscopic techniques and evaluated in vitro for the antimicrobial, antifungal, as well as antitubercular activity. Among all the synthesized derivatives, compounds 6b, 6d, 6e, 6g, and 6j demonstrated excellent antimicrobial activity on Bacillus subtilis. The compounds 6d, 6j and compounds 6b, 6f, 6h, and 6i exhibited maximum zone of inhibition against fungi Candida albicans as well as Aspergillus niger, respectively at the concentration of 500 μg/mL. The antitubercular activity exhibited by 6f, 6g, and 6d with minimum inhibitory concentration (MIC) values of 1.2, 3.1, and 7.8 μg/mL, respectively. The synthesized compounds were studied by molecular docking through Autodock Vina to evaluate their interaction at respective proteins. Further the effect of synthesized derivatives on surface morphology of human erythrocytes as well as hemolysis was also evaluated. The results demonstrated lesser extent of hemolytic toxicity.

Antimicrobial activities of synthetic arylidine nicotinic and isonicotinic hydrazones

Background: Despite availability of variety of antibacterial agents, re-emergance of pathogenic bacteria is still a serious medical concern. Identification of new, safer, and selective antibacterial agents is the key interest in the medicinal chemistry research. Methods: A library of synthetic arylidene nicotinic and isonicotinic hydrazones (1-63) were investigated for antimicrobial activities. Results: A number of derivatives showed significant to moderate antimicrobial activities against Gram positive and Gram negative bacterial cultures. Few compounds also showed antifungal activity against fungal cultures. Minimum Inhibitory Concentration (MIC) was calculated for the most active compounds 1, 7, 11, 19, 34, 46, 50, 51, and 55 against gram positive and gram negative cultures. Conclusion: Newly identified compounds may serve as lead for future research in order to get the more powerful antibacterial agents.

Xanthine oxidase inhibitory activity of nicotino/isonicotinohydrazides: A systematic approach from in vitro, in silico to in vivo studies

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

METHOD FOR PREPAREING 1,3,4-OXADIAZOL UNDER SOLVENT-FREE CONDITION

The present invention relates to a synthesis method of 1,3,4-oxadiazol, comprising: 1) under a solvent-free condition and by means of a mechanical pulverization method, making a hydrazide compound react with an aldehyde compound and thereby synthesizing a N-acylhydrazone compound; and 2) under a solvent-free condition, adding an iodine-based oxidizing agent to the N-acylhydrazone compound to synthesize 1,3,4-oxadiazol via oxidative cyclization. The solventless synthesis method of 1,3,4-oxadiazol according to the present invention is easy to perform and handle, and has the advantage of synthesizing 1,3,4-oxadiazol at high selectivity and yield. Also, the solventless synthesis method of the present invention can prevent the formation of side products caused by the minute amount of water that usually remains in solvents, and can further prevent synthesized intermediates from being converted back into the starting materials by the water.COPYRIGHT KIPO 2016

Synthesis, antimycobacterial, antiviral, antimicrobial activities, and QSAR studies of nicotinic acid benzylidene hydrazide derivatives

A series of nicotinic acid benzylidene hydrazide derivatives (1-18) was synthesized and tested in vitro for biological evaluations. The antimycobacterial activity results indicated that the presence of electron-withdrawing halogen groups at para position of the phenyl ring improved their activity. The results of antiviral evaluation depicted that none of the synthesized derivatives inhibited the replication of viruses at subtoxic concentration. Further, the antimicrobial screening results indicated that compounds having OCH3 and NO2 substituents were the most active ones. QSAR investigations revealed that multitarget QSAR models were effective in describing the antimicrobial activity. Springer Science+Business Media, LLC 2011.

Synthesis and analgesic activity of new pyridine-based heterocyclic derivatives

A series of new heterocyclic derivatives having a pyridine nucleus were synthesized. 4-(5-(2-Chlorophenyl)- 4H-1,2,4-triazol-3-yl)pyridine (7c) and 4-(5-(2- Nitrophenyl)-4H-1,2,4-triazol-3-yl)pyridine (7d) presented the best analgesic profie of this series in hot-plate, tail-flick, and formalin-induced licking tests, which was partially prevented by pretreatment with mecamylamine, a nicotinic receptor antagonist. Springer Science+Business Media, LLC 2010.

Mechanistic differences between in vitro assays for hydrazone-based small molecule inhibitors of anthrax lethal factor

A systematically generated series of hydrazones were analyzed as potential inhibitors of anthrax lethal factor. The hydrazones were screened using one UV-based and two fluorescence-based in vitro assays. The study identified several inhibitors with IC50 values in the micromolar range, and importantly, significant differences in the types of inhibition were observed with the different assays.