Abstract

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.