Development of 2‐Alkyl‐5‐((phenylsulfonyl)oxy)‐1H‐indole‐3‐carboxylate Derivatives as Potential Anti‐Biofilm Agents

Abstract

A series of novel 2-alkyl-5-((phenylsulfonyl)oxy)-1H-indole-3carboxylate derivatives were synthesized and evaluated for their cytotoxicity, antibacterial and anti-biofilm activities. Some of these compounds were able to inhibit biofilm formation of the tested strains with biofilm inhibitory concentration in the range of 12.5-50 μM. The results indicated N-methylpiperazine moiety was the key factor affecting the compound's activity. Compounds 5 l and 5 m with F substituent at the phenyl ring at 5-position of indole ring, presented the most potent biofilm inhibitory activity (more than 90 % inhibition percentage) against E. faecalis 16C51 at biofilm inhibitory concentration (12.5 μM). Furthermore, compounds 5 f and 5 h with Br/CH 3 substituent at the phenyl ring at 1-position of indole ring, showed the greatest biofilm inhibitory activity (more than 85 % inhibition percentage) against MRSA YUSA145 at biofilm inhibitory concentration (12.5 μM).

Indole-Acrylonitrile Derivatives as Potential Antitumor and Antimicrobial Agents—Synthesis, In Vitro and In Silico Studies

“…The importance of the indole skeleton to date has led to the development of diverse bioactive compounds that have been identified with anti-inflammatory [6,7], antioxidant and cytoprotective [8,9], antidepressant [10], anti-migraine [11], antihypertensive [12], antidiabetic [13,14] or antiviral [15] effects and as antitubercular agents [16]. Moreover, indole derivatives represent a significant source of novel antibacterial agents that may exhibit their biological activity through the inhibition of Pharmaceuticals 2023, 16, 918 2 of 35 efflux pumps, biofilm or filamentous temperature-sensitive protein Z (FtsZ), and methicillinresistant Staphylococcus aureus pyruvate kinase [17][18][19][20][21][22].…”

“…Pharmaceuticals 2023, 16, 918 2 of 34 as antitubercular agents [16]. Moreover, indole derivatives represent a significant source of novel antibacterial agents that may exhibit their biological activity through the inhibition of efflux pumps, biofilm or filamentous temperature-sensitive protein Z (FtsZ), and methicillin-resistant Staphylococcus aureus pyruvate kinase [17][18][19][20][21][22]. Particular attention has been paid to indole-containing compounds with anticancer properties, which exert their activity by affecting numerous biological targets [23][24][25].…”