Abstract
Using a routine procedure, a number of derivatives of the benzo[4,5]isothiazolo[2,3-a]pyrazine-6,6-dioxide ring system have been synthesized from readily available starting materials. A series of chalcones were synthesized, which were subsequently reacted with chlorosulfonic acid to generate chalcone sulfonyl chlorides. The chalcone sulfonyl chlorides were then treated with bromine to generate dibromo chalcone sulfonyl chlorides. These were subsequently reacted with 1,2-diaminopropane and 2-methyl-1,2-diaminopropane in boiling ethanol resulting in compounds 2–10 and 11–19 respectively, in 12–80% yields. The products were characterized by spectral analysis and the definitive structure of compound 11 was determined by X-ray crystallography. The synthesized compounds were screened for potential antibacterial properties against Bacillus subtilis, Escherichia coli, Proteus vulgaris and Staphylococcus aureus.
Highlights
Antibacterial resistance has provoked an urgent need for novel antimicrobial agents
The synthesis started with substituted acetophenones reported extensively overby thereacting last fifty3,4-dimethoxybenzaldehyde years [19]
The chalcones number of patents report synthetic routes to the aisothiazolo[2,3-a]pyrazine ring system were initially reacted with chlorosulfonic acid to yield the sulfonyl chlorides which were subsequently
Summary
Antibacterial resistance has provoked an urgent need for novel antimicrobial agents. There has been a significant decline in the number of new antibacterial agents being released onto the market [1]. In 2012, researchers synthesized group, of which two of the compounds displayed promising activity as potential 5-HT6 antagonists a group of benzoisothiazole derivatives that contained an N,N-dimethylformamide group, of which [14]. Pyrazine derivatives have andbeen colleagues synthesized of twenty which extensively reviewed ainlibrary the literature [16] benzimidazole-1,3,4-oxadiazole and have displayed a wide range derivatives of antimicrobial showed anti-tuberculosis activity at concentrations as low as μg [15]. The synthesis started with by reacting 3,4-dimethoxybenzaldehyde with substituted acetophenones reacted the withknown bromine in glacialmethod acetic acid the dibromochalcone chlorides These following literature to resulting generatein a number of chalconessulfonyl [22].
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