Nader S. Abutaleb
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View article: Repurposing epetraborole to combat <i>Neisseria gonorrhoeae</i> and <i>Chlamydia trachomatis</i> infections
Repurposing epetraborole to combat <i>Neisseria gonorrhoeae</i> and <i>Chlamydia trachomatis</i> infections Open
Neisseria gonorrhoeae and Chlamydia trachomatis are the most common bacterial sexually transmitted infections. The World Health Organization (WHO) estimates that there were approximately 211 million cases of chlamydia and gonorrhea in 2020…
View article: Discovery of Novel Probiotic Species to Improve Infant Health 2349
Discovery of Novel Probiotic Species to Improve Infant Health 2349 Open
Description Selecting the right infant formula can be challenging for parents due to the wide range of options, often resulting in suboptimal choices or frequent changes. Our recent studies in mice have shown that the maternal microbiota, …
View article: Discovery of Novel Probiotic Species to Improve Infant Health
Discovery of Novel Probiotic Species to Improve Infant Health Open
Selecting an appropriate infant formula can be challenging for parents given the wide range of available options, which may lead to suboptimal choices or frequent switching. Our recent studies in mice demonstrated that the maternal microbi…
View article: Halogenated N-(1,3,4-oxadiazol-2-yl) benzamides are effective eradicators of methicillin-resistant Staphylococcus aureus biofilms
Halogenated N-(1,3,4-oxadiazol-2-yl) benzamides are effective eradicators of methicillin-resistant Staphylococcus aureus biofilms Open
Due to the ever-increasing threat of methicillin-resistant Staphylococcus aureus (MRSA), we have embarked on a campaign to discover novel antibacterial agents which are effective at eradicating both MRSA, as well as acting on pre-formed MR…
View article: Hit-to-Lead Optimization of Acetazolamide-Based Bacterial Carbonic Anhydrase Inhibitors with Efficacy In Vivo for Treatment of Vancomycin-Resistant Enterococci Septicemia
Hit-to-Lead Optimization of Acetazolamide-Based Bacterial Carbonic Anhydrase Inhibitors with Efficacy In Vivo for Treatment of Vancomycin-Resistant Enterococci Septicemia Open
As one of the leading causes of hospital-acquired infections reported by the National Healthcare Safety Network, vancomycin-resistant enterococci (VRE) continue to afflict patients in healthcare facilities, with limited FDA-approved drugs …
View article: A novel peptide mimetic, brilacidin, for combating multidrug-resistant Neisseria gonorrhoeae
A novel peptide mimetic, brilacidin, for combating multidrug-resistant Neisseria gonorrhoeae Open
Neisseria gonorrhoeae is classified by the Centers for Disease Control and Prevention as an urgent public health threat due to rising infections and rapid resistance development. N. gonorrhoeae has developed resistance to nearly all FDA-ap…
View article: Redesigning oxazolidinones as carbonic anhydrase inhibitors against vancomycin-resistant enterococci
Redesigning oxazolidinones as carbonic anhydrase inhibitors against vancomycin-resistant enterococci Open
The rise of vancomycin-resistant enterococci (VRE) as a leading cause of hospital-acquired infections underscores the urgent need for new treatment strategies. In fact, resistance has developed not only to vancomycin but also to other clin…
View article: Optimization of Ethoxzolamide Analogs with Improved Pharmacokinetic Properties for <i>In Vivo</i> Efficacy against <i>Neisseria gonorrhoeae</i>
Optimization of Ethoxzolamide Analogs with Improved Pharmacokinetic Properties for <i>In Vivo</i> Efficacy against <i>Neisseria gonorrhoeae</i> Open
Drug-resistant gonorrhea is caused by the bacterial pathogen Neisseria gonorrhoeae, for which there is no recommended oral treatment. We have demonstrated that the FDA-approved human carbonic anhydrase inhibitor ethoxzolamide potent…
View article: Development of Penicillin-Based Carbonic Anhydrase Inhibitors Targeting Multidrug-Resistant <i>Neisseria gonorrhoeae</i>
Development of Penicillin-Based Carbonic Anhydrase Inhibitors Targeting Multidrug-Resistant <i>Neisseria gonorrhoeae</i> Open
The development of antibacterial drugs with new mechanisms of action is crucial in combating the rise of antibiotic-resistant infections. Bacterial carbonic anhydrases (CAs, EC 4.2.1.1) have been validated as promising antibacterial target…
View article: Novel phenylthiazoles with a <i>tert</i>-butyl moiety: promising antimicrobial activity against multidrug-resistant pathogens with enhanced ADME properties
Novel phenylthiazoles with a <i>tert</i>-butyl moiety: promising antimicrobial activity against multidrug-resistant pathogens with enhanced ADME properties Open
The structure–activity relationship of a new tert -butylphenylthiazole series, with a pyrimidine linker, was investigated.
View article: Inhibition of pathogenic bacterial carbonic anhydrases by monothiocarbamates
Inhibition of pathogenic bacterial carbonic anhydrases by monothiocarbamates Open
Carbonic anhydrases (CAs) from the pathogenic bacteria Nesseria gonorrhoeae and vancomycin-resistant enterococci (VRE) have recently been validated as antibacterial drug targets. Here we explored the inhibition of the α-CA from N…
View article: Discovery of 1,2-diaryl-3-oxopyrazolidin-4-carboxamides as a new class of MurA enzyme inhibitors and characterization of their antibacterial activity
Discovery of 1,2-diaryl-3-oxopyrazolidin-4-carboxamides as a new class of MurA enzyme inhibitors and characterization of their antibacterial activity Open
View article: Substituted salicylic acid analogs offer improved potency against multidrug-resistant Neisseria gonorrhoeae and good selectivity against commensal vaginal bacteria
Substituted salicylic acid analogs offer improved potency against multidrug-resistant Neisseria gonorrhoeae and good selectivity against commensal vaginal bacteria Open
View article: Lopinavir and ritonavir act synergistically with azoles against Candida auris in vitro and in a mouse model of disseminated candidiasis
Lopinavir and ritonavir act synergistically with azoles against Candida auris in vitro and in a mouse model of disseminated candidiasis Open
View article: Substituted salicylic acid analogs offer improved potency against multidrug-resistant Neisseria gonorrhoeae and good selectivity against commensal vaginal bacteria
Substituted salicylic acid analogs offer improved potency against multidrug-resistant Neisseria gonorrhoeae and good selectivity against commensal vaginal bacteria Open
Drug-resistant Neisseria gonorrhoeae represents a major threat to public health; without new effective antibiotics, untreatable gonococcal infections loom as a real possibility. In a previous drug-repurposing study, we reported that salicy…
View article: Evaluation of 1,3,4-Thiadiazole Carbonic Anhydrase Inhibitors for Gut Decolonization of Vancomycin-Resistant Enterococci
Evaluation of 1,3,4-Thiadiazole Carbonic Anhydrase Inhibitors for Gut Decolonization of Vancomycin-Resistant Enterococci Open
Vancomycin-resistant enterococci (VRE), Enterococcus faecium and Enterococcus faecalis, are high-priority drug-resistant pathogens in need of new therapeutic approaches. VRE originate in the gastrointestinal tract of carriers…
View article: Exploring novel aryl/heteroaryl-isosteres of phenylthiazole against multidrug-resistant bacteria
Exploring novel aryl/heteroaryl-isosteres of phenylthiazole against multidrug-resistant bacteria Open
Twenty-three compounds of novel phenylthiazole derivatives were synthesized utilizing the Suzuki coupling reaction. Antibacterial activity in an in vivo model against MRSA USA300 was evaluated, as it reduced the burden of MRSA USA300 in sk…
View article: Naphthylthiazoles: a class of broad-spectrum antifungals
Naphthylthiazoles: a class of broad-spectrum antifungals Open
Cryptococcal infections remain a major cause of mortality worldwide due to the ability of Cryptococci to pass through the blood–brain barrier (BBB) causing lethal meningitis.
View article: Expanding the structure–activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents
Expanding the structure–activity relationships of alkynyl diphenylurea scaffold as promising antibacterial agents Open
With the continuous and alarming threat of exhausting the current antimicrobial arsenals, efforts are urgently needed to develop new effective ones.
View article: Isoquinoline Antimicrobial Agent: Activity against Intracellular Bacteria and Effect on Global Bacterial Proteome
Isoquinoline Antimicrobial Agent: Activity against Intracellular Bacteria and Effect on Global Bacterial Proteome Open
A new class of alkynyl isoquinoline antibacterial compounds, synthesized via Sonogashira coupling, with strong bactericidal activity against a plethora of Gram-positive bacteria including methicillin- and vancomycin-resistant Staphylococcu…
View article: Structure-activity relationship studies for inhibitors for vancomycin-resistant <i>Enterococcus</i> and human carbonic anhydrases
Structure-activity relationship studies for inhibitors for vancomycin-resistant <i>Enterococcus</i> and human carbonic anhydrases Open
Vancomycin-resistant enterococci (VRE), consisting of pathogenic Enterococcus faecalis and E. faecium, is a leading cause of hospital-acquired infections (HAIs). We recently repurposed the FDA-approved human carbonic anhydrase (CA) …
View article: Mechanistic Studies and <i>In Vivo</i> Efficacy of an Oxadiazole-Containing Antibiotic
Mechanistic Studies and <i>In Vivo</i> Efficacy of an Oxadiazole-Containing Antibiotic Open
Methicillin-resistant Staphylococcus aureus (MRSA) infections are still difficult to treat, despite the availability of many FDA-approved antibiotics. Thus, new compound scaffolds are still needed to treat MRSA. The oxadiazole-conta…
View article: Auranofin exerts antibacterial activity against Neisseria gonorrhoeae in a female mouse model of genital tract infection
Auranofin exerts antibacterial activity against Neisseria gonorrhoeae in a female mouse model of genital tract infection Open
Neisseria gonorrhoeae has been classified by the U.S. Centers for Disease Control and Prevention as an urgent threat due to the rapid development of antibiotic resistance to currently available antibiotics. Therefore, there is an urgent ne…
View article: In vivo efficacy of acetazolamide in a mouse model of Neisseria gonorrhoeae infection
In vivo efficacy of acetazolamide in a mouse model of Neisseria gonorrhoeae infection Open
View article: Repurposing FDA-approved sulphonamide carbonic anhydrase inhibitors for treatment of <i>Neisseria gonorrhoeae</i>
Repurposing FDA-approved sulphonamide carbonic anhydrase inhibitors for treatment of <i>Neisseria gonorrhoeae</i> Open
Neisseria gonorrhoeae is a high-priority pathogen of concern due to the growing prevalence of resistance development against approved antibiotics. Herein, we report the anti-gonococcal activity of ethoxzolamide, the FDA-approved hum…
View article: Dithiocarbamates effectively inhibit the α-carbonic anhydrase from <i>Neisseria gonorrhoeae</i>
Dithiocarbamates effectively inhibit the α-carbonic anhydrase from <i>Neisseria gonorrhoeae</i> Open
Recently, inorganic anions and sulphonamides, two of the main classes of zinc-binding carbonic anhydrase inhibitors (CAIs), were investigated for inhibition of the α-class carbonic anhydrase (CA, EC 4.2.1.1) from Neisseria gonorrhoeae
View article: Evaluation of bisphenylthiazoles as a promising class for combating multidrug-resistant fungal infections
Evaluation of bisphenylthiazoles as a promising class for combating multidrug-resistant fungal infections Open
To minimize the intrinsic toxicity of the antibacterial agent hydrazinyloxadiazole 1 , the hydrazine moiety was replaced with ethylenediamine (compound 7 ). This replacement generated a potent antifungal agent with no antibacterial activit…
View article: Nanocapsules modify membrane interaction of polymyxin B to enable safe systemic therapy of Gram-negative sepsis
Nanocapsules modify membrane interaction of polymyxin B to enable safe systemic therapy of Gram-negative sepsis Open
Nanocapsules modify membrane interaction of polymyxin B to reduce its toxicity and enable safe systemic therapy of sepsis.
View article: Investigating auranofin for the treatment of infected diabetic pressure ulcers in mice and dermal toxicity in pigs
Investigating auranofin for the treatment of infected diabetic pressure ulcers in mice and dermal toxicity in pigs Open
View article: In vitro and in vivo activities of the carbonic anhydrase inhibitor, dorzolamide, against vancomycin-resistant enterococci
In vitro and in vivo activities of the carbonic anhydrase inhibitor, dorzolamide, against vancomycin-resistant enterococci Open
Vancomycin-resistant enterococci (VRE) are a serious public health threat and a leading cause of healthcare-associated infections. Bacterial resistance to antibiotics recommended for the treatment of enterococcal infections complicates the…