Synthesis, physico-chemical properties of 2-((4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)acetohyd-razides
Journal Title: Фармацевтичний журнал - Year 2016, Vol 5, Issue 5
Abstract
The value of the class of 1,2,4-triazole derivatives to create a low-toxic and highly active substances is huge. There are a lot of facts about the high biological activity among a number of substances. The 2-((4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)acetohydrazides derivatives causes of particular interest in this direction. The aim of the work was to synthesize 2-((4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)acetohydrazides and their derivatives, studying of their physico-chemical properties. 2-((4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)-N'-R-acetohydrazides were synthesized by of 2-((4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)acetohydrazides with aldehydes and ketones in the i-propanol with the addition of hydrochloric acid. The melting point was determined by an automatic device for determining the melting point OptiMelt Stanford Research Systems MPA100 (US). The elemental composition of compounds found in elemental analyzer Elementar Vario L cube (CHNS) (standard ‒ sulfonamides). Chromatography-mass spectral studies conducted on gas-liquid chromatograph Agilent 1260 Infinity HPLC with equipped mass spectrometer Agilent 6120, 1H-NMR-spectra were registered on spectrometer Mercury 400 A series of new 2-((4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)-N'-R-acetohydrazides derivatives were synthesized, R-2-chloro-6-fluorobenzylidene, 3-nitrobenzylidene, 4-hydroxybenzylidene, 2-nitrobenzylidene, 2,4-dimethylbenzylidene, 3,5-dimethoxybenzylidene, 3-bromo-4-fluorobenzylidene, 2,3-dimethoxybenzylidene, 2-bromobenzylidene, 2-fluorobenzylidene, 4-(dimethylamino)benzylidene, pyridin-2-ylmethylene, 5-nitrofuran-2-ylmethylene, 4-methoxybenzylidene, 2-hydroxybenzylidene, 4-methoxyphenyl)ethylidene, 1-(thiophen-2-yl)ethylidene. The structure of these compounds was established by modern physico-chemical analysis methods (elemental analysis, 1H-NMR spectroscopy). Individuality was proved by HPLC-MS.
Authors and Affiliations
A. A. Safonov
The studing of antimicrobial activity of 4-(R-ylidenamino)-3-( morpholinomethylene)-4H-1,2,4-triazole-5-thiol
According to the information of the World Health Organization (WHO) the lethal cases caused by pathogenic microorganisms occupied the one of the leading places. Most acutely the problem posed in countries where economic...
Study of microbiological purity with myramistin, anesthezine and CO2 extract of chamomile for use in surgical practice
Any finished dosage forms, including soft dosage forms, are subject to microbial contamination. It can be caused by microbial contamination of plant-based medicinal raw materials, air, industrial premises, equipment, ute...
Use of modeling in the study of economic burden of influenza in the elderly population in Central and Eastern European countries
The economic burden of the incidence of influenza and ARI requires careful study, since annually about 15% of the world's population suffers from these diseases. In addition, the flu can cause complications that are dang...
Comparative analysis of topical dermatologic drugs with corticosteroids in the markets of Ukraine and Russian Federation
One of the most top medical and social problems of contemporaneity is spreading of skin inflammatory diseases of. Main place in the treatment of dermatological diseases takes topical dermatological therapy, by using drug...
Medical and pharmaceutical law: features of palliative care to the pharmaceutical correction of patients with pain syndromes
Reform of the modern health care system is aimed at improving access to medicines for patients of different clinical and pharmacological classification, regulatory and legal nomenclature groups. It acquires special impor...