Antibacterial and anti-quorum sensing activities of a substituted thiazole derivative against methicillin-resistant Staphylococcus aureus and other multidrug-resistant bacteria

Ibrahim, Yasser Musa; Abouwarda, Ahmed Megahed; Nasr, Tamer; Omar, Farghaly A.; Bondock, Samir

doi:10.1016/j.micpath.2020.104500

Cited by 23 publications

(8 citation statements)

References 42 publications

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“…[ 66 ] Ibrahim et al synthesized 5‐acetyl‐4‐methyl‐2‐(3‐pyridyl) thiazole for evaluating antimicrobial activity and demonstrated several interactions with Gln164, Arg190, and Lys154 as −4.6526 kcal/mol binding energy. [ 67 ] 1‐hydroxy‐1‐norresistomycin was evaluated against human clinical pathogens by Ramalingam et al in vivo and in vitro. The docking score of the molecule, which significantly influences the biofilm formation, with SarA was recorded as −4.38 kcal/mol.…”

Section: Resultsmentioning

confidence: 99%

Antimicrobial and antibiofilm activities and bovine serum albumin binding properties of benzimidazolium derivative NHC salts and their Ag(I)‐NHC complexes

Çelik

Üstün

Şahin

et al. 2022

Applied Organom Chemis

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Benzimidazole type N‐heterocyclic carbene molecules and their metal complexes have well‐known biological activity. Elemental silver and silver complexes also have antibacterial and antifungal activity. In this study, silver complexes with 1‐allyl 5,6‐dimethylbenzimidazolium derivative ligands were analyzed for their antimicrobial and antibiofilm activities. Additionally, bovine serum albumin (BSA) binding properties of the molecules were analyzed by spectrophotometric methods, and the details of interactions of the molecules with BSA were investigated by molecular docking methods. While N‐heterocyclic carbene salts showed moderate antifungal and antibiofilm activity, silver complexes of these salts have strong antimicrobial activity with <1.9–15.6 μg/ml minimal inhibitory concentration (MIC) values. On the other hand, carbene salts have better affinity against BSA than the complexes. Additionally, the interaction of the optimized complexes with SarA and BSA were analyzed by molecular docking methods. According to in vitro and in silico evaluation, the studied Ag complexes may be utilized for advanced studies.

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Section: Resultsmentioning

confidence: 99%

Antimicrobial and antibiofilm activities and bovine serum albumin binding properties of benzimidazolium derivative NHC salts and their Ag(I)‐NHC complexes

Çelik

Üstün

Şahin

et al. 2022

Applied Organom Chemis

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“…Rishirilide A ( 45 ) is a plasmin antagonist with a highly oxygenated anthracene skeleton which is produced by Streptomyces rishiriensis OFR-1056 ( Figure 2 D) [ 42 ]. As depicted in Figure 3 D, Rishirilide A did not display a significant growth inhibitory activity against E. faecalis up to a 35 µM concentration.…”

Section: Resultsmentioning

confidence: 99%

“…The supernatant was collected by centrifugation at 16,600× g for 10 min and the optical density (OD) was measured at 543 nm [ 41 ]. The anti-hemolysin activity of the tested compounds was determined by comparing the hemolytic activity of S. aureus cultured with/without the investigated compounds and then calculating the ratio [ 42 ]. The experiment was performed in triplicate.…”

Section: Methodsmentioning

confidence: 99%

Secondary Metabolites of Actinomycetales as Potent Quorum Sensing Inhibitors Targeting Gram-Positive Pathogens: In Vitro and In Silico Study

et al. 2022

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Anti-virulence agents are non-bacteriostatic and non-bactericidal emerging therapeutic options which hamper the production of virulence factors in pathogenic flora. In Staphylococcus aureus and Enterococcus faecalis, regulation of virulence genes’ expression occurs through the cyclic peptide-mediated accessory gene regulator (agr) and its ortholog fsr quorum sensing systems, respectively. In the present study, we screened a set of 54 actinomycetales secondary metabolites as novel anti-virulence compounds targeting quorum sensing system of the Gram-positive bacteria. The results indicated that four compounds, Phenalinolactones A–D, BU–4664LMe, 4,5-dehydrogeldamycin, and Questinomycin A, potentially inhibit the agr quorum sensing system and hemolytic activity of S. aureus. On the other hand, Decatromicin A and B, Okilactomycin, Rishirilide A, Abyssomicin I, and Rebeccamycin selectively blocked the fsr quorum sensing system and the gelatinase production in E. faecalis at sub-lethal concentrations. Interestingly, Synerazol uniquely showed the capability to inhibit both fsr and agr quorum sensing systems. Further, in silico molecular docking studies were performed which provided closer insights into the mode of action of these compounds and proposed that the inhibitory activity of these compounds could be attributed to their potential ability to bind to the ATP-active site of S. aureus AgrA. Taken together, our study highlights the potential of actinomycetales secondary metabolites with diverse structures as anti-virulence quorum sensing inhibitors.

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“…Thiazole ring is widely recognized as scaffold of great value for obtaining molecules endowed with potent antibacterial and anti‐biofilm properties [15,43] . Recently, the 5‐acetyl‐4‐methyl‐2‐(3‐pyridyl) thiazole 4 (Figure 6) was found able to interfere with the QS system as well as with the production of virulence factors including biofilm formation [44] . The antivirulence effects were evaluated on the clinical isolates MRSA−C18 and MRSA−C91, which are known for their multidrug‐resistance and their strong biofilm forming capacity.…”

Section: Mrsa Biofilm Developmentmentioning

confidence: 99%

Therapeutic Strategies To Counteract Antibiotic Resistance in MRSA Biofilm‐Associated Infections

et al. 2020

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Methicillin‐resistant Staphylococcus aureus (MRSA) has emerged as one of the leading causes of persistent human infections. This pathogen is widespread and is able to colonize asymptomatically about a third of the population, causing moderate to severe infections. It is currently considered the most common cause of nosocomial infections and one of the main causes of death in hospitalized patients. Due to its high morbidity and mortality rate and its ability to resist most antibiotics on the market, it has been termed a “superbug”. Its ability to form biofilms on biotic and abiotic surfaces seems to be the primarily means of MRSA antibiotic resistance and pervasiveness. Importantly, more than 80 % of bacterial infections are biofilm‐mediated. Biofilm formation on indwelling catheters, prosthetic devices and implants is recognized as the cause of serious chronic infections in hospital environments. In this review we discuss the most relevant literature of the last five years concerning the development of synthetic small molecules able to inhibit biofilm formation or to eradicate or disperse pre‐formed biofilms in the fight against MRSA diseases. The aim is to provide guidelines for the development of new anti‐virulence strategies based on the knowledge so far acquired, and, to identify the main flaws of this research field, which have hindered the generation of new market‐approved anti‐MRSA drugs that are able to act against biofilm‐associated infections

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Antibacterial and anti-quorum sensing activities of a substituted thiazole derivative against methicillin-resistant Staphylococcus aureus and other multidrug-resistant bacteria

Cited by 23 publications

References 42 publications

Antimicrobial and antibiofilm activities and bovine serum albumin binding properties of benzimidazolium derivative NHC salts and their Ag(I)‐NHC complexes

Antimicrobial and antibiofilm activities and bovine serum albumin binding properties of benzimidazolium derivative NHC salts and their Ag(I)‐NHC complexes

Secondary Metabolites of Actinomycetales as Potent Quorum Sensing Inhibitors Targeting Gram-Positive Pathogens: In Vitro and In Silico Study

Therapeutic Strategies To Counteract Antibiotic Resistance in MRSA Biofilm‐Associated Infections

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