Design and synthesis of oxaprozin-1,3,4-oxadiazole hybrids as potential anticancer and antibacterial agents |
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| Authors: | Parsharamulu Rayam Naveen Polkam Naveen Kuntala Venkanna Banothu Hasitha Shilpa Anantaraju Yogeeswari Perumal Sridhar Balasubramanian Jaya Shree Anireddy |
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| Affiliation: | 1. Centre for Chemical Sciences and Technology, IST, Jawaharlal Nehru Technological University Hyderabad, Kukatpally, Hyderabad, Telangana State, India;2. Department of Biotechnology, IST, Jawaharlal Nehru Technological University Hyderabad, Kukatpally, Hyderabad, Telangana State, India;3. Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Hyderabad, Telangana State, India;4. X-ray Crystallography Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, Telangana State, India |
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| Abstract: | In the present study, we report design, synthesis and screening of new novel 5-substituted-2-mercapto-1,3,4-oxadiazole analogues appended to oxaprozin for their in vitro anticancer and antibacterial activity. The synthesised compounds were characterized using various spectroscopic techniques. Furthermore, the structure of 5b (2-(2-[4,5-diphenyloxazol-2-yl]ethyl)-5-(ethylthio)-1,3,4-oxadiazole) was unequivocally confirmed by X-ray analysis. Among the series 5c (2-(2-[4,5-diphenyloxazol-2-yl]ethyl)-5-(propylthio)-1,3,4-oxadiazole) showed most promising anticancer activity against A549 cancer cell line and all the reported analogues manifested satisfactory safety profiles against human normal cell line HEK293T. The products exhibited good antibacterial activity and among the tested 5j (2-(2-[4,5-diphenyloxazol-2-yl]ethyl)-5-([4-fluorobenzyl]thio)-1,3,4-oxadiazole) exhibited most potent. |
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