A novel pyrimidine derivatives with aryl urea, thiourea and sulfonamide moieties: Synthesis, anti-inflammatory and antimicrobial evaluation

作者：Keche Ashish P; Hatnapure Girish D; Tale Rajesh H; Rodge Atish H; Birajdar Satish S; Kamble Vandana M^*

来源：Bioorganic & Medicinal Chemistry Letters, 2012, 22(10): 3445-3448.

DOI：10.1016/j.bmcl.2012.03.092

• Pyrimidine
• Urea
• Thiourea and sulfonamide derivatives
• Anti-inflammatory
• Anti-bacterial
• Anti-fungal

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-alpha 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-alpha and 56-96% IL-6 inhibitory activity) with reference to standard dexamethasone at 10 mu M. 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.

• 出版日期2012-5-15