Synthesis, physical and chemical properties and anxiolytic activity OF 2-(4-(R-arylidenamino)-5-methyl-4H-1,2,4-triazole-3-YL)thio)acetic acids and their salts
Journal Title: ScienceRise: Pharmaceutical Science - Year 2018, Vol 0, Issue 3
Abstract
<p>It is estimated that 50% of all molecules of medicinal products used in drug therapy are administered as salts. This fact indicates that formation of a medicinal substance salt is an important stage in the development of a medicinal remedy.</p><p>Therefore, we believe that the combinatorial synthesis of organic and inorganic salts of derivatives of 1,2,4-triazole has not only theoretical but also practical significance.</p><p><strong>The aim of the work </strong>is to synthesize and establish the structure of new 2-((4-(R-arylidenamino)-5-methyl-4H-1,2,4-triazole-3-yl)thio)acetic acids and their salts, where R is 2H, 4-dimethylaminobenzyliden, 2-hydroxybenzyliden, 4-hydroxybenzyliden, 4-nitrobenzyliden and their anxiolytic activity.</p><p><strong>Materials and methods of research.</strong><strong> </strong>The physical and chemical properties of the obtained compounds were examined according to the methods presented in the State Pharmacopoeia of Ukraine. The melting temperature was determined on an automatic melting device OptiMelt Stanford Research Systems MPA100 (US production). The elemental composition of the compounds was installed on the elemental analyzer Elementar Vario EL cube (CHNS) (standard - sulfanilamide). Chromatographic mass spectral studies were performed on a gas-liquid chromatograph Agilent 1260 Infinity HPLC equipped with an Agilent 6120 mass spectrometer (ionization in an electrical spray (ESI), <sup>1</sup>H NMR spectra were recorded on a Mercury 400 spectrometer, DMSO-D<sub>6</sub> solvent, internal standard - tetramethylsilane.</p><p>Anxiogenic and anxiolytic activities of the studied compounds in the S. Pellow test.</p><p><strong>Research results</strong><strong>. </strong>4-(R-arylideneamino)-5-methyl-4H-1,2,4-triazole-3-thiols were taken as initial materials, where R was 2H, 4-dimethylaminobenzylidene, 2-hydroxybenzylidene, 4-hydroxybenzylidene, 4-nitrobenzylidene.</p><p>Synthesis of 4-(R-arylideneamino)-5-methyl-4H-1,2,4-triazole-3-thiols, where R was 4-dimethylaminobenzylidene, 2-hydroxybenzylidene, 4-hydroxybenzylidene, 4-nitrobenzylidene, was conducted by adding aromatic aldehyde (4-dimethylaminobenzaldehyde, 2-hydroxybenzaldehyde, 4-hydroxybenzaldehyde, 4-nitrobenzaldehyde) to 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol in acetate acid and heated to dissolution of sediment.</p><p>The preparation of 2-((4-(R-arylidenamino)-5-methyl-4H-1,2,4-triazole-3-yl)thio)acetic acids was carried out by adding an aromatic aldehyde to an equivalent amount of 2-((4-amino)-5-methyl-4H-1,2,4-triazole-3-yl)thio)acetic acid in acetic acid medium when heated.</p><strong>Conclusions. </strong>A series of new 2-((4-(R-arylidenamino)-5-methyl-4H-1,2,4-triazole-3-yl)thio)acetic acids were synthesized. The structure of synthesized compounds was established using modern physical and chemical methods of analysis. Some physical and chemical properties of the obtained substances were researched
Authors and Affiliations
Yevgean Pruglo
Keywords
Related Articles
- EP ID EP526835
- DOI 10.15587/2519-4852.2018.135786
- Views 157
- Downloads 0
Вивчення летких фракцій сировини рогозу вузьколистого (Typha angustifolia L.)
<p>Рогіз вузьколистий – поширена в багатьох країнах світу, зокрема в Україні, рослина. Дана рослина застосовується для лікування різноманітних захворювань, а саме циститу, уретриту, використовують її як антиоксидантний,...
Algorithm for carrying out a procedure for verification of a spectrophotometric method for analysis of solid-dosed dosage forms according to the requirements of SPHU 2.0
<p><strong>Aim</strong><strong>. </strong>The increase in the pharmaceutical market of Ukraine of the range of medicines leads to stricter requirements for their quality. According to the requirements of international st...
Study of the morphologo-anatomic signs of shoots of the Salix caprea L. of Ukrainian flora
<p>Representatives of the Salicaceae family are valuable sources of medicinal plant material that has long been used in traditional medicine in many countries around the world. In European countries, some willow species...
Дослідження компонентів летких фракцій рослинної сировини салату посівного сорту «Лолло Россо»
<p>Рослини є важливим джерелом одержання біологічно активних речовин, які проявляють різноманітну фармакологічну активність. Увагу привертають не лише рослини, які традиційно використовуються з лікувально-профілактичною...
Визначення сертиндолу у біологічному матеріалі методом газової хроматографії – мас-спектрометрії
<p>Лікування антипсихотичним препаратом нового покоління сертиндолом при передозуванні чи комбінуванні його з деякими лікарськими засобами, супроводжується пролонгацією QT інтервалу та злоякісним нейролептичним синдромом...