Call For Paper Volume:7 Issue:2 Feb'2020 |

One-pot regioselective synthesis of some new benzothiazine-isoxazole hybrids and their in vitro, in silico anti-bacterial evaluation.

Publication Date : 14/02/2020


DOI : 10.21884/IJMTER.2020.7008.O4AKY

Author(s) :

Satheesh kumar Nukalaa , M Ravinder , T Savitha Jyostna.


Volume/Issue :
Volume 7
,
Issue 2
(02 - 2020)



Abstract :

The one-pot regioselective synthesis of few novel benzothiazine-isoxazole hybrids (5a-5j) through the Cu(I) promoted 1,3-dipolarcycloaddition between 4-(prop-2-ynyl)-2H-benzo[b][1,4]thiazin-3(4H)-one and in situ formed aromatic nitrile oxides in benign aqueous butanol media at room temperature was described. All the newly prepared compounds were characterized by 1H NMR, 13C NMR and mass spectral data & further screened for their in vitro antibacterial activity against a panel of Gram-positive Bacillus Sphaericus and Staphylococcus Epidermidis and Gram-negative KlebsiellaPneumoniae and Escherichia Coli species. Few of the synthesized compounds like 5e, 5h, 5i and 5j have been found to shown potent growth inhibition activity as compared to commercial standard drugs Penicillin-G and Streptomycin. Molecular docking with beta-ketoacyl-acyl carrier protein synthase III( PDB ID-1HNJ) revealed that the compounds 5e, 5h have interaction with the protein with binding energies -11.12 Kcal/mol and -11.07 Kcal/mol respectively.


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One-pot regioselective synthesis of some new benzothiazine-isoxazole hybrids and their in vitro, in silico anti-bacterial evaluation.

February 9, 2020