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Title: Synthesis and antibacterial evaluation of benzazoles tethered dihydro[1,3]oxazines
Authors: Prasad, Davinder
Rohilla, Rajesh Kumar
Roy, Nilanjan
Nath, Mahendra
Keywords: One-pot methodology;Antibacterial efficacy;Benzazoles;Dihydro[1,3]oxazines;Polymerization
Issue Date: May-2012
Publisher: NISCAIR-CSIR, India
Abstract: Synthesis of various benzazoles tethered 1,3-oxazines such as 1H-benzo[d]azolophenyl-3,4-dihydro-2H-benzo­[e][1,3]oxazines 2a-j, 2-(3-(1H-benzo[d]oxazol-2-yl)phenyl)-2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazine 3, 2-(3-(1H-benzo-[d]imidazol-2-yl)phenyl)-2,3-dihydro-1H-naphtho[1,2-e][1,3]oxazine 4 and 3-(3-(benzo[d]oxazol-2-yl)phenyl)-7-(benzo[d]thiazol-2-yl)-3,4-dihydro-2H-benzo[e][1,3]oxazine 5 has been accomplished through three-component one-pot Mannich type condensation-cyclization reaction of substituted phenols or β-naphthol with formaldehyde and benzazolo­phenyl amines at 80-90°C. All the newly synthesized compounds have been characterized on the basis of elemental and spectral analyses. Moreover, these compounds have been evaluated for their in vitro antibacterial efficacy against two Gram-positive bacteria viz S. epidermidis and S. aureus and two Gram-negative bacteria viz E. coli and P. aeruginosa. Interestingly, the compounds, 2f-i have displayed significant antibacterial efficacy with IC50 (0.208-1.106 µg/mL).
Page(s): 739-745
ISSN: 0975-0983(Online); 0376-4699(Print)
Appears in Collections:IJC-B Vol.51B(05) [May 2012]

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