Main-chain flexibility and hydrophobicity of ionenes strongly impact their antimicrobial activity: an extended study on drug resistance strains and Mycobacterium

Abstract

A high significance of the main chain flexibility and an unexpected effect of hydrophobicity on the biological activity in series of ionenes was observed. The most potent among the tested polycations showed high activity toward clinical bacterial isolates.

Enhanced Synergistic Antibacterial and Antibiofilm Efficacy of Main-Chain Polysulfoniums with Antibiotics by Balancing Charge Density and Amphiphilicity

“…By mimicking the natural antimicrobial peptides (AMPs), main-chain cation-containing polymers have emerged as a promising alternative to conventional antibiotics. 11 They access the structural benefit of antimicrobial membrane rupturing properties from AMPs but with low production costs and high proteolytic stability. 12 Different from polymeric antimicrobials residing with positively charged groups, mainchain cationic polymers usually have a characteristic of precise alternating sequences, and the cationic moieties sitting in the backbone can be easily facilitated to insert the hydrophobic segments into the phospholipid bilayers of bacterial cell membranes.…”

“…By mimicking the natural antimicrobial peptides (AMPs), main-chain cation-containing polymers have emerged as a promising alternative to conventional antibiotics . They access the structural benefit of antimicrobial membrane rupturing properties from AMPs but with low production costs and high proteolytic stability .…”

A fluorescent quaternary phosphonium main-chain-type polymer: an opportunity to fabricate functional materials with excellent antibacterial activity and bacterial imaging capability

“…8,9 Tailoring polymeric formulas has been explored as an effective way to overcome the challenge of antimicrobial resistance, especially main-chain (MC)-type cationic polymers have been documented as better alternatives than side-chain (SC) polymers and small molecule cationic compounds. 8,[10][11][12][13] In MC cationic polymers, the positively charged hydrophilic segments and hydrophobic carbon chains are alternatively integrated into the polymeric backbone. 14,15 These structures are similar to antimicrobial peptides, enabling excellent attractions between the negatively charged bacterial surface and the cationic hydrophilic groups and hydrophobic regions.…”

Investigation of Naphthyl–Polyamine Conjugates as Antimicrobials and Antibiotic Enhancers

“…Drug development issues associated with HDPs, including susceptibility to proteolysis, high production costs, and, in some case, low to moderate activity under physiological salt conditions, prevent their direct introduction as clinical agents [ 8 ]. In order to overcome these deficiencies, an extensive amount of research has been directed towards the synthesis and biological evaluation of synthetic mimics of antimicrobial peptides, so-called SMAMPs [ 9 , 10 , 11 , 12 , 13 , 14 , 15 ]. Numerous different structural classes of SMAMPs have been identified, including shorter peptides (e.g., LTX-109 ( 1 )), sterols (e.g., squalamine ( 2 )), and hydantoins (e.g., 3 ) ( Figure 1 ) [ 15 , 16 , 17 ].…”

“…Antibiotics 2023, 12, x FOR PEER REVIEW 2 of 26 mimics of antimicrobial peptides, so-called SMAMPs [9][10][11][12][13][14][15]. Numerous different structural classes of SMAMPs have been identified, including shorter peptides (e.g., LTX-109 (1)), sterols (e.g., squalamine (2)), and hydantoins (e.g., 3) (Figure 1) [15][16][17].…”