Synthesis of 6-oxopyrimidin-1(6H)-yl benzamide derivatives and evaluation of their antibacterial and cytotoxic activity |
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| Authors: | Kiran Devarasetty Giri Tharikoppula Tailor Sridhar Laxminarayana Eppakayala Mahesh Kyasani Premkumar Arumugam |
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| Institution: | 1. Chemistry Services Unit, GVK Biosciences Pvt. Ltd., Hyderabad, India;2. Chemistry Division, Institute of Science and Technology, JNT University, Hyderabad, India;3. Department of Chemistry, Sreenidhi Institute of Science and Technology (Autonomous), Hyderabad, India |
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| 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 oxadiazolo3,2-a]pyrimidin-5-one and evaluated for their antibacterial and cytotoxicity. Most of the compounds exhibited antibacterial activity. In particular, compounds 5b and 5k exhibited considerable antibiotic activity against Klebsiella pneumonia and Bacillus cereus. In addition, compounds 5g and 5i also inhibited the growth of two human tumor cell lines (A549 and H460) at micromolar concentrations. |
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| Keywords: | Cancer cell lines cytotoxic agents fused oxadiazole oxadiazolo[3 2-a]pyrimidin-5-ol oxadiazolo[3 2-a]pyrimidin-5-one pyrimidines |
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