ANTI MYCOBACTERIAL ACTIVITY OF 1, 4-OXAZINES AND 1, 4- THIAZINES
Sindhu T. J.*, David Paul, Meena Chandran, A R Bhat, K Krishnakumar
ABSTRACT
Tuberculosis is the world’s second most common cause of death from
infectious disease, after HIV/ AIDS. The disease is usually chronic
with varying clinical manifestation, remains one of the biggest public
health problems in the 21st century. The present study was designed to
synthesise some novel derivatives of 1, 4-oxazines and 1, 4- thiazines
by using O-aminophenol and O-amino thiophenol with maleic
anhydride respectively. Further 8 Mannich bases were synthesised
from 3-oxo-3, 4-dihydro-2h-1, 4-benzoxazin-2-yl) acetic acid and 3-
oxo-3, 4-dihydro-2H-1, 4-benzothiazin-2-yl) acetic acid with sulpha
drugs, ethanol and formaldehyde. Then the synthesised Mannich bases
were screened for their antimycobacterial activity by using Micro plate
Alamar Blue Assay (MABA). The results indicate the Mannich bases
of 1, 4-thiazines and the Mannich bases of 1, 4 oxazines have considerable antimycobacterial
activity. Out of the 8 derivatives, 4b (Sulfamethoxazole substituted 1, 4- thiazine) is most
effective and showing activity at 25μg/ml. The study suggests that 1, 4-Thiazine derivatives
shows potent antimycobacterial activity than 1, 4-Oxazine derivatives.
Keywords: Tuberculosis, Oxazine, Thiazine, MABA method.
[Download Article]
[Download Certifiate]