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

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• 作者：Ashish P. Keche^a ; Girish D. Hatnapure^a ; Rajesh H. Tale^c ; Atish H. Rodge^c ; Satish S. Birajdar^a ; Vandana M. Kamble^a ; ^b ; ^{m.vandana248@gmail.com}
• 关键词：Pyrimidine ; Urea ; Thiourea and sulfonamide derivatives ; Anti-inflammatory ; Anti-bacterial ; Anti-fungal
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 May, 2012
• 卷：22
• 期：10
• 页码：3445-3448
• 文件大小：238 K

摘要

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 (dFont">1-dFont">25) were screened for their pro-inflammatory cytokines (TNF-伪 and IL-6) and antimicrobial activity (antibacterial and antifungal). Biological data revealed that among all the compounds screened, compounds dFont">5, dFont">6, dFont">11, dFont">12, dFont">16 and dFont">20 were found to have moderate to potent anti-inflammatory activity (up to 48-78%TNF-伪 and 56-96%IL-6 inhibitory activity) with reference to standard dexamethasone at 10 渭M. The compounds dFont">10, dFont">12, dFont">13, dFont">18, dFont">20, dFont">22, dFont">24 and dFont">25 found to have promising antimicrobial activity against all the selected pathogenic bacteria and fungi.