Synthesis and Biological Activity of Guanidine Scaffold: A Comprehensive Review

Abstract:: 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.