Synthesis of 6-oxopyrimidin-1(6H)-yl benzamide derivatives and evaluation of their antibacterial and cytotoxic activity. Issue 3 (1st February 2016)

• Record Type: Journal Article
• Authors: Devarasetty, Kiran; Tharikoppula, Giri; Sridhar, Tailor; Eppakayala, Laxminarayana; Kyasani, Mahesh; Arumugam, Premkumar; Pusuluri, Srinivas
• Is Part Of: Synthetic communications. Volume 46:Issue 3(2016)
• Page Start: 263
• Page End: 274
• Publication Date: 2016-02-01
• Subjects: Cancer cell lines -- cytotoxic agents -- fused oxadiazole -- oxadiazolo[3, 2-a]pyrimidin-5-ol -- oxadiazolo[3, 2-a]pyrimidin-5-one -- pyrimidines; Organic compounds -- Synthesis -- Periodicals; Chemistry, Organic; Synthesis; 547.205
• DOI: 10.1080/00397911.2015.1135349
• Languages: English
• ISSNs: 0039-7911

Abstract

ABSTRACT: A series of novel 2-alkylamino and 2, 4-dialkyl amino 6-oxopyrimidin-1(6H)-yl) benzamide derivatives were prepared in good yields from a base-catalyzed ring opening of oxadiazolo[3, 2-a]pyrimidin-5-one and evaluated for their antibacterial and cytotoxicity. Most of the compounds exhibited antibacterial activity. In particular, compounds5b and5k exhibited considerable antibiotic activity against Klebsiella pneumonia and Bacillus cereus . In addition, compounds5g and5i also inhibited the growth of two human tumor cell lines (A549 and H460) at micromolar concentrations. GRAPHICAL ABSTRACT: