title: The novel 3,4-dihydropyrimidin-2(1H)-one urea derivatives of N-aryl urea: synthesis, anti-inflammatory, antibacterial and antifungal activity evaluation.
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.
authors: Department of Chemistry, School of Chemical Sciences, Swami Ramanand Teerth University (SRTM), Nanded, India. rkht_2008@rediffmail.com
authors: Rajesh H
authors: RH
authors: Tale
authors: Atish H
authors: AH
authors: Rodge
authors: Girish D
authors: GD
authors: Hatnapure
authors: Ashish P
authors: AP
authors: Keche
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015850:Interleukin-6 / Q000378:metabolism; D008826:Microbial Sensitivity Tests; D011744:Pyrimidinones / Q000737:chemistry*; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors / Q000378:metabolism; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000093242:Interleukin-6 Inhibitors
chemical_list: D000900:Anti-Bacterial Agents; D000893:Anti-Inflammatory Agents; D000935:Antifungal Agents; D015850:Interleukin-6; D011744:Pyrimidinones; D014409:Tumor Necrosis Factor-alpha; D014508:Urea; D000093242:Interleukin-6 Inhibitors