Synthesis, biological evaluation and docking study of some novel isoxazole clubbed 1,3,4-oxadiazoles derivatives

A novel series of isoxazole clubbed 1,3,4-oxadiazole derivatives have been synthesized by reaction of 5-(3-fluoro-4-methoxyphenyl) isoxazole-3-carbohydrazide with different substituted benzoic/pyridinyl/indolyl acids in phosphorous oxychloride, characterized by IR, 1 H NMR, 13 C NMR, MS analytical d...

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Veröffentlicht in:Medicinal chemistry research 2018-04, Vol.27 (4), p.1283-1291
Hauptverfasser: Shingare, Ramesh M., Patil, Yogesh S., Sangshetti, Jaiprakash N., Patil, Rajesh B., Rajani, Dhanji P., Madje, Balaji R.
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Sprache:eng
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Zusammenfassung:A novel series of isoxazole clubbed 1,3,4-oxadiazole derivatives have been synthesized by reaction of 5-(3-fluoro-4-methoxyphenyl) isoxazole-3-carbohydrazide with different substituted benzoic/pyridinyl/indolyl acids in phosphorous oxychloride, characterized by IR, 1 H NMR, 13 C NMR, MS analytical data and evaluated for their antimicrobial as well as antitubercular activity. Antibacterial activity of compounds 5e , 5g , 5h , 5j and 5l were found to be good against E. coli, P. aeruginosa, S. aureus and S. pyogenes as compared to standard Ampicillin. Compound 5b and 5i were found to be active antitubercular agents against M. tuberculosis H37Rv. Antibacterial and antitubercular activity was supported by molecular docking to gain insights of the mode of inhibition of MurD ligase enzyme.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-018-2148-2