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Design and synthesis of oxaprozin‐1,3,4‐oxadiazole hybrids as potential anticancer and antibacterial agents
Author(s) -
Rayam Parsharamulu,
Polkam Naveen,
Kuntala Naveen,
Banothu Venkanna,
Anantaraju Hasitha Shilpa,
Perumal Yogeeswari,
Balasubramanian Sridhar,
Anireddy Jaya Shree
Publication year - 2020
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3842
Subject(s) - oxadiazole , chemistry , antibacterial activity , combinatorial chemistry , cancer cell lines , thio , in vitro , stereochemistry , cell culture , cancer cell , cancer , organic chemistry , biochemistry , bacteria , medicine , genetics , biology
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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