The novel 3,4-dihydropyrimidin-2(1H)-one urea derivatives of N-aryl urea: synthesis, anti-inflammatory, antibacterial and antifungal activity evaluation |
| |
Authors: | Tale Rajesh H Rodge Atish H Hatnapure Girish D Keche Ashish P |
| |
Institution: | a Department of Chemistry, School of Chemical Sciences, Swami Ramanand Teerth University (SRTM), Nanded, India b Department of Chemistry, Udaygiri Mahavidayla, Udgir, India |
| |
Abstract: | A series of novel 3,4-dihydropyrimidin-2(1H)-one urea derivatives of biological interest were prepared by sequential Bigineli’s reaction, reduction followed by reaction of resulting amines with different arylisocynates. All the synthesized (1-23) compounds were screened against the pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Biological activity evaluation study reveled that among all the compounds screened, compounds 12 and 17 found to have promising anti-inflammatory activity (68-62% TNF-α and 92-86% IL-6 inhibitory activity at 10 μM). Interestingly compounds 3, 4, 5, 6, 15, 22 and 23 revealed promising antimicrobial activity at MIC of 10-30 μg/mL against selected pathogenic bacteria and fungi. |
| |
Keywords: | 3 4-Dihydropyrimidin-2(1H)-ones Urea derivatives Anti-inflammatory Anti-bacterial Anti-fungal |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|