Novel Synthesis and Antimicrobial Activities of Thiazino-Oxazine Derivatives

Abstract

In the designing and synthesis of new heterocyclic compounds, containing two different pharmacophores, we have carried out new series of 3-(4-chlorophenyl)-4-methylidene-4,8-dihydro-2H,5H-1,3-thiazino[5,4-e]-1,3-oxazine-2,5,7(3H)-trione derivatives (5a-5k) in good yields from the cyclization of 5-[(1E)-N- (4-chlorophenyl) ethanimidoyl] -4-hydroxy- 2H-1,3- thiazine-2,6(3H)-dione derivatives (4a-4k) with triphosgene. All the synthesized compounds (5a-5k) were confirmed by spectral analysis. The synthesized compounds (5a-5k) were screened in vitro for their antibacterial activities against S. subtilis (gram positive) and E. coli. (gram negative) while antifungal activity against C. albicans by cup plate method. Some of the products of series were found to have quite good activities as compared to the standard drug streptomycin and flucanozole.

Fully Selective Synthesis of Spirocyclic-1,2-oxazine N-Oxides via Non-Catalysed Hetero Diels-Alder Reactions with the Participation of Cyanofunctionalysed Conjugated Nitroalkenes

“…It is interesting that based on the herbicidal testing, oxazine derivatives possessed excellent herbicidal activity agents at the root of radish, grain sorghum, rape, cucumber and barnyard grass [ 22 ]. This class of compounds show high herbicidal activity on a wide variety of grasses and significant safety in cereals, rice, soybeans, and corn in preemergence tests [ 23 ]. Generally, the universal strategy for constructing six-membered organic rings is the Diels-Alder (DA) reaction [ 24 ].…”