Synthesis of Piperidine Conjugated Quinoxalines as Potential Antibiofilm Agents

Abstract

aims: N-(1-benzylpiperidin-4-yl)quinoxalin-2-amines were synthesized and evaluated for antisalmonella activity against S. paratyphi. background: The most common cause of foodborne illness is bacterial or viral contamination. Although there are several therapeutics available to combat against these microbes, they lost their efficacy in long term medication. Because, over a period of time microbes developed a resistance against the drugs and this antimicrobial resistance is a serious threat to global public health as a consequence widely disseminated and careless use of antimicrobials. Therefore, there is a need to develop some new chemical moieties with a safety factor and better efficacy. A series of substituted N-(1-benzylpiperidin-4-yl)quinoxalin-2-amines (5a-j) (5ab, 5ac) were synthesized and screened for their in-vitro antibacterial activity against Salmonella paratyphi, a well-known food borne pathogen. objective: N-(1-benzylpiperidin-4-yl)quinoxalin-2-amines were synthesized and evaluated for antisalmonella activity against S. paratyphi. method: Experimental methods, Agar well diffusion and Broth microdilution assays were carried out to evaluate the antibacterial activity of the lead compounds. Further antibiofilm methods, Crystal violet and MTT assays were subjected to investigate their biofilm inhibition capacity against S. paratyphi. result: Among tested compounds, 5b, 5e, 5h and 5j bearing 4-chloro, 3,4-dimethoxy, 4-methyl and thienyl groups on phenyl ring of quinoxalines were emerged as potential candidates having a significant antisalmonella activity. In these four potential candidates, compounds 5b and 5h effective against salmonella whereas compounds 5e and 5j effectively inhibited the biofilm formation of salmonella. conclusion: N-(1-benzylpiperidin-4-yl)quinoxalin-2-amines (5a-j) (5ab, 5ac) were synthesized and evaluated for antisalmonella activity against S. paratyphi. Among series of compounds, four compounds significantly showed good activity and emerged as antibacterial agents for further studies in future. other: Nil