SYNTHESIS AND PRIMARY SCREENING OF ANTI-INFLAMMATORY ACTIVITY OF 1,4,5,6-TETRAHYDROPYRIMIDINE-2-CARBOXAMIDES

• Main Authors: V. Ya. Horishny, D. A. Frolov, I. O. Nektegayev, Yu. V. Ostapiuk, V. S. Matiychuk
• Format: Article
• Language: English
• Published: Ukrmedknyha Publishing House 2018-06-01
• Series: Фармацевтичний часопис
• Subjects: органічний синтез; піримідин; тіоксоацетамід; тіазол; морфолін; протизапальна активність.
• Online Access: https://ojs.tdmu.edu.ua/index.php/pharm-chas/article/view/9125
• ISSN: 2312-0967; 2414-9926

The aim of the work. Development of methods for obtaining new morpholin-4-yl-2-thioxoacetamides and investigate their reaction with 1,3-diaminopropane; synthesis of new 1,4,5,6-tetrahydropyrimidine-2-carboxamides and primary screening of their anti-inflammatory properties. Materials and Methods. Organic synthesis, NMR spectroscopy, elemental analysis, pharmacological screening. Results and Discussion. By the reaction of chloroacetamides with sulfur and morpholine a series of 2-morpholin-4-yl-2-thioxoacetamides were synthesized. They were investigated in the reaction with 1,3-diaminopropane. As a result, the series of new 1,4,5,6-tetrahydropyrimidine-2-carboxamides were prepared. The anti-inflammatory activity of some synthesized compounds has been investigated. Conclusions. The method of synthesis of 1,4,5,6-tetrahydropyrimidine-2-carboxamides was developed. The results of anti-inflammatory activity investigation of synthesized compounds allowed us to identify highly active derivatives which was appropriate to the reference non-steroidal antiinflammatory drug “Diclofenac Sodium” by indicator of inhibition of inflammatory reaction (37.5–46.7 %).