Pharmaceutical Approaches on Antimicrobial Resistance: Prospects and Challenges

Nainu, Firzan; Permana, Andi Dian; Djide, Natsir; Anjani, Qonita Kurnia; Utami, Rifka Nurul; Rumata, Nur Rahma; Zhang, Jianye; Emran, Talha Bin; Simal-Gándara, Jesús

doi:10.3390/antibiotics10080981

Cited by 34 publications

(17 citation statements)

References 215 publications

(273 reference statements)

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“…It was hypothesized that these diamides (and triamides) could behave as unnatural peptidomimetics mimicking the overall amphipathic structures and hence could have a mechanism of action similar to antimicrobial peptides [ 61 , 62 ]. Therefore, triamides based on the structure of active diamides were tested for their antimicrobial activity, and their zero antibacterial effect was a complete disappointment.…”

Section: Resultsmentioning

confidence: 99%

Study of Biological Activities and ADMET-Related Properties of Salicylanilide-Based Peptidomimetics

Pindjakova

Pilařová

Pauk

et al. 2022

IJMS

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A series of eleven benzylated intermediates and eleven target compounds derived from salicylanilide were tested against Staphylococcus aureus ATCC 29213 and Enterococcus faecalis ATCC 29212 as reference strains and against three clinical isolates of methicillin-resistant S. aureus (MRSA) and three isolates of vancomycin-resistant E. faecalis. In addition, the compounds were evaluated against Mycobacterium tuberculosis H37Ra and M. smegmatis ATCC 700084. The in vitro cytotoxicity of the compounds was assessed using the human monocytic leukemia cell line THP-1. The lipophilicity of the prepared compounds was experimentally determined and correlated with biological activity. The benzylated intermediates were found to be completely biologically inactive. Of the final eleven compounds, according to the number of amide groups in the molecule, eight are diamides, and three are triamides that were inactive. 5-Chloro-2-hydroxy-N-[(2S)- 4-(methylsulfanyl)-1-oxo-1-{[4-(trifluoromethyl)phenyl]amino}butan-2-yl]benzamide (3e) and 5-chloro-2-hydroxy-N-[(2S)-(4-methyl-1-oxo-1-{[4-(trifluoromethyl)phenyl]amino)pentan-2-yl)benzamide (3f) showed the broadest spectrum of activity against all tested species/isolates comparable to the used standards (ampicillin and isoniazid). Six diamides showed high antistaphylococcal activity with MICs ranging from 0.070 to 8.95 μM. Three diamides showed anti-enterococcal activity with MICs ranging from 4.66 to 35.8 μM, and the activities of 3f and 3e against M. tuberculosis and M. smegmatis were MICs of 18.7 and 35.8 μM, respectively. All the active compounds were microbicidal. It was observed that the connecting linker between the chlorsalicylic and 4-CF3-anilide cores must be substituted with a bulky and/or lipophilic chain such as isopropyl, isobutyl, or thiabutyl chain. Anticancer activity on THP-1 cells IC50 ranged from 1.4 to >10 µM and increased with increasing lipophilicity.

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Section: Resultsmentioning

confidence: 99%

Study of Biological Activities and ADMET-Related Properties of Salicylanilide-Based Peptidomimetics

Pindjakova

Pilařová

Pauk

et al. 2022

IJMS

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“…The activity of these compounds against Gram-negative, glucose non-fermenting rods has already been assessed in previous studies. As noted by Nainu et al, CSA-131 is a good bactericidal and anti-biofilm agent against Pseudomonas aeruginosa, and in combination with colistin, it also acts against Acinetobacter baumannii CRAB (carbapenem-resistant) strains [43]. The latest research by Oyardi et al, carried out with 40 strains of S. maltophilia isolated from patients suffering from cystic fibrosis also indicates that CSA-131 and CSA-131P (delivered with Pluronik F-127) can be considered effective antibacterial and anti-biofilm agents against S. maltophilia [20]; results that agree well with our findings.…”

Section: Discussionmentioning

confidence: 95%

Bactericidal Activity of Ceragenin in Combination with Ceftazidime, Levofloxacin, Co-Trimoxazole, and Colistin against the Opportunistic Pathogen Stenotrophomonas maltophilia

et al. 2022

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Background: Stenotrophomonas maltophilia (S. maltophilia) is an emerging opportunistic Gram-negative rod causing nosocomial infections predominantly in immunocompromised patients. Due to its broad intrinsic resistance to antibiotics, including carbapenems and the ability to form a biofilm, it is difficult to eradicate. Methods: In this study, the benefit of combined administration (potential synergism) and anti-biofilm activity of ceragenins: CSA-13, CSA-44, and CSA-131 (synthetic mimics of natural antimicrobial peptides) with ceftazidime, levofloxacin, co-trimoxazole and colistin against clinical strains of S. maltophilia were determined using MIC/MBC (minimum inhibitory concentration/minimum bactericidal concentration), killing assays and CV staining. Results: Obtained data indicate that the ceragenins exhibit strong activity against the tested strains of S. maltophilia grown in planktonic culture and as stationary biofilms. Moreover, with some strains, the synergy of ceragenins with conventional antibiotics was observed Conclusion: Our data suggest that ceragenins are promising agents for future development of new methods for treatment of infections caused by S. maltophilia, along with its potential use in combination with conventional antibiotics.

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“…Using the Schiff base reaction, a thermo-responsive hydrogel of Pluronic F127, poly(ε-lysine) and hyaluronic acid was used for loading an antibacterial photocatalyst, used for continuous sterilization and bacteria-infected wound healing [118]. Many efforts are focused on alternatives to antibiotics and bacterial resistant materials [119].…”

Section: Biological Propertiesmentioning

confidence: 99%

Bioinspired Hydrogels as Platforms for Life-Science Applications: Challenges and Opportunities

Bercea¹

2022

Polymers

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Hydrogels, as interconnected networks (polymer mesh; physically, chemically, or dynamic crosslinked networks) incorporating a high amount of water, present structural characteristics similar to soft natural tissue. They enable the diffusion of different molecules (ions, drugs, and grow factors) and have the ability to take over the action of external factors. Their nature provides a wide variety of raw materials and inspiration for functional soft matter obtained by complex mechanisms and hierarchical self-assembly. Over the last decade, many studies focused on developing innovative and high-performance materials, with new or improved functions, by mimicking biological structures at different length scales. Hydrogels with natural or synthetic origin can be engineered as bulk materials, micro- or nanoparticles, patches, membranes, supramolecular pathways, bio-inks, etc. The specific features of hydrogels make them suitable for a wide variety of applications, including tissue engineering scaffolds (repair/regeneration), wound healing, drug delivery carriers, bio-inks, soft robotics, sensors, actuators, catalysis, food safety, and hygiene products. This review is focused on recent advances in the field of bioinspired hydrogels that can serve as platforms for life-science applications. A brief outlook on the actual trends and future directions is also presented.

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Pharmaceutical Approaches on Antimicrobial Resistance: Prospects and Challenges

Cited by 34 publications

References 215 publications

Study of Biological Activities and ADMET-Related Properties of Salicylanilide-Based Peptidomimetics

Study of Biological Activities and ADMET-Related Properties of Salicylanilide-Based Peptidomimetics

Bactericidal Activity of Ceragenin in Combination with Ceftazidime, Levofloxacin, Co-Trimoxazole, and Colistin against the Opportunistic Pathogen Stenotrophomonas maltophilia

Bioinspired Hydrogels as Platforms for Life-Science Applications: Challenges and Opportunities

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