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 |
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Hauptverfasser: | , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
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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. |
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ISSN: | 1054-2523 1554-8120 |
DOI: | 10.1007/s00044-018-2148-2 |