The indole motif plays a significant role in the quest for innovative drugs. As proposed, novel N‐substituted indole derivatives were synthesized, and their efficacy against bacteria and fungi was evaluated in vitro. The synthesis of these compounds was confirmed using easily accessible building blocks, and their structural formulas were supported by corrected analytical and spectroscopic analyses. Fresh strains of Candida albicans, Escherichia coli, and Pseudomonas aeruginosa, as well as Bacillus subtilis and Staphylococcus aureus, were utilized to assess the antibacterial and antifungal activities. Notably, the derivatives 1‐(phenyl (piperidine‐1‐yl) methyl)‐1H‐indole and 4‐(1H‐indol‐1‐yl) (phenyl) morpholine have strong antifungal effects on Candida albicans that are equivalent to those of the widely used drug fluconazole.