title: A novel pyrimidine derivatives with aryl urea, thiourea and sulfonamide moieties: synthesis, anti-inflammatory and antimicrobial evaluation.
abstract: A series of novel 4-(3-(trifluoromethyl)phenylamino-6-(4-(3-arylureiodo/arylthioureido/arylsulfonamido)-pyrimidine derivatives of biological interest were prepared by the sequential Suzuki cross coupling, acid amination, reduction followed by reaction of resulting amine with different arylisocyantes or arylisothiocyantes or arylsulfonyl chlorides. All the synthesized compounds (1-25) were screened for their pro-inflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Biological data revealed that among all the compounds screened, compounds 5, 6, 11, 12, 16 and 20 were found to have moderate to potent anti-inflammatory activity (up to 48-78% TNF-α and 56-96% IL-6 inhibitory activity) with reference to standard dexamethasone at 10 μM. The compounds 10, 12, 13, 18, 20, 22, 24 and 25 found to have promising antimicrobial activity against all the selected pathogenic bacteria and fungi.
authors.affiliation: Department of Chemistry, Maharashtra Udaygiri Mahavidayla, Udgir, India.
authors.forename: Ashish P
authors.initials: AP
authors.lastname: Keche
authors.forename: Girish D
authors.initials: GD
authors.lastname: Hatnapure
authors.forename: Rajesh H
authors.initials: RH
authors.lastname: Tale
authors.forename: Atish H
authors.initials: AH
authors.lastname: Rodge
authors.forename: Satish S
authors.initials: SS
authors.lastname: Birajdar
authors.forename: Vandana M
authors.initials: VM
authors.lastname: Kamble
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013449:Sulfonamides / Q000737:chemistry; D013890:Thiourea / Q000737:chemistry; D014508:Urea / Q000737:chemistry
chemical_list: D000890:Anti-Infective Agents; D000893:Anti-Inflammatory Agents; D011743:Pyrimidines; D013449:Sulfonamides; D014508:Urea; D013890:Thiourea