Synthesis and Biological Activity of Guanidine Scaffold: A Comprehensive Review

Derivatives of guanidine are found to be highly informative for their design in antibacterial and anticancer applications, thus positioning them as promising future drug candidates. This study evaluates and synthesizes a diverse group of guanidine derivatives, with a focus on those bearing cyclic aryl and acyl groups. The prepared compounds showed strong antifungal and antibacterial activities with selectivity against Candida albicans and Gram-positive bacteria. The Structure-Activity Relationship analysis showed that substituent groups are important for biological activity, and n-propyl linkages achieved an optimal balance between hemolytic and antibacterial properties. Additionally, the antiproliferative activities of all synthesized compounds (110a-110v) were assessed in Michigan Cancer Foundation-7 (MCF-7) human breast cancer cells. The Structure Activity Relationship study results suggest that planned substitutions can significantly enhance biological activity, offering potential approaches to counter the growing threat of antibiotic resistance.