Tigecycline is an important antibacterial drug for treating infection by clinical multidrug-resistant bacteria, and tigecycline-resistant Staphylococcus aureus (TRSA) has been increasingly reported in recent years. Notably, only rpsJ mepA are associated with the tigecycline resistance of S. aureus. The gene encodes MepA efflux pumps, overexpression confirmed to be directly related resistance. Although mutations widely occur, associations between TRSA still unclear. In this study, we explored...

Abstract Objectives To evaluate the in vitro and vivo antimicrobial activity of pleuromutilin derivatives modified with C14 side-chain against Streptococcus suis. Methods determine minimum inhibitory concentrations (MICs) 268 modifications S. suis ATCC 43 765 using broth dilution method. Derivative B43, B49, B52, B53 B54, which exhibited better activity, were selected for further investigation their antibacterial effect, cytotoxicity, effect. Results Determination five clinical strains (n =...

Abstract Objectives To investigate the epidemiology of fosB-positive Staphylococcus aureus in waterfowl farms Pearl River tributaries Guangdong Province, China 2020. Methods A total 63 S. were recovered from 315 samples collected six duck and one goose farm. PFGE, WGS analysis performed on 19 aureus. Results The fosfomycin resistance rate strains was as high 52.4% (33/63), 30.1% (19/63) carried fosB. Resistance gene prediction results showed that farm environment-derived contained...

Background: Bacterial infections cause a serious public health crisis due to the emergence of resistance towards multiple conventional antibacterial drugs. In particular, multidrug-resistant (MDR) Enterococcus faecium which belongs "ESKAPE" organisms is causing significant problems worldwide. Hence, there an urgent need find alternative therapies. Recently, substituted benzene guanidine compounds have been used as lead structures discover new promising drugs in both synthetic and medicinal...

Introduction: Riemerella anatipestifer (R. anatipestifer) is an important pathogen in waterfowl, leading to substantial economic losses. In recent years, there has been a notable escalation the drug resistance rate of R. anatipestifer. Consequently, imperative need expedite development novel antibacterial medications effectively manage infection caused by . Methods: This study investigated vitro and vivo activities substituted benzene guanidine analog, namely, isopropoxy (IBG), against using...

Staphylococcus aureus, especially methicillin-resistant S. aureus (MRSA), is an important zoonotic microorganism that increasingly causes public health concern worldwide. The objective of this study was to determine the prevalence and transmission in duck farms evaluate its antimicrobial resistance genetic characteristics.

Serious infections caused by multidrug-resistant Staphylococcus aureus clearly urge the development of new antimicrobial agents. Drug repositioning has emerged as an alternative approach that enables us to rapidly identify effective drugs. We first reported a guanidine compound, isopropoxy benzene guanidine, had potent antibacterial activity against S. aureus. Unlike conventional antibiotics, repeated use lower probability resistance section. found triggered membrane damage disrupting cell...

Plasmid-borne colistin resistance mediated by mcr-1 is a growing problem, which poses serious challenge to the clinical application of for Gram-negative bacterial infections. Drug combination one effective strategies treat colistin-resistant bacteria. Here, we found guanidine compound, namely, isopropoxy benzene (IBG), boosted efficacy against mcr-1-positive Salmonella. This study aimed develop pharmacokinetics/pharmacodynamics (PK/PD) model combining with IBG Salmonella in an intestinal...

Isopropoxy benzene guanidine (IBG) is a novel substituted analogue with antibacterial activity against multidrug-resistant bacteria. However, the bioavailability of IBG not optimal due to its finite aqueous solubility, thus hampering potential therapeutic exploitation. In this study, we prepared IBG/hydroxypropyl-β-CD (IBG/HP-β-CD) complex, and characterized it by differential scanning calorimetry, Fourier transform infrared spectroscopy, powder X-ray diffraction, electron microscopy....

Isopropoxy benzene guanidine (IBG) is a derivative with antibacterial activity against multidrug-resistant bacteria. A few studies have revealed the metabolism of IBG in animals. The aim current study was to identify potential metabolic pathways and metabolites IBG. detection characterization were performed high-performance liquid chromatography tandem mass spectrometry (UHPLC-Q-TOF-MS/MS). Seven identified from microsomal incubated samples by using UHPLC-Q-TOF-MS/MS system. rat liver...

Bovine mastitis caused by infectious pathogens can lead to a decline in production performance and an increase elimination rate, resulting huge losses the dairy industry. This study aims prepare novel cow teat disinfectant with polyhexamethylene biguanide (PHMB) as main bactericidal component evaluate its activity vitro disinfection effect teats. PHMB concentration of 3 g/L was prepared PVA-1788, propylene glycol glycerol excipients. When dilution ratio is 1:4800 action time 5 min, reduce...

The phenylpyrazole derivative 5-amino-3-[1-cyano-2-(3-phenyl-1H-pyrazol-4-yl) vinyl]-1-phenyl-1H-pyrazole-4-carbonitrile (LN002), which was screened out through high-throughput molecular docking for the AOX target, exhibits promising efficacy against Cryptosporidium. However, its poor water solubility limits oral bioavailability and therapeutic utility. In this study, solid dispersion agents were prepared by using HP-β-CD Soluplus® characterized differential scanning calorimetry, Fourier...

Cryptosporidiosis is considered a crucial zoonotic disease caused by widely distributing parasitic protozoa called

This study aimed to evaluate the antibacterial activity of isopropoxy benzene guanidine (IBG) against C. perfringens based on pharmacokinetics/pharmacodynamics (PK/PD) modeling in broilers. The PK parameters IBG plasma and ileal content perfringens-infected broilers following oral administration at 2, 30, 60 mg/kg body weight were investigated. vivo PD studies conducted over ranging from 2 repeated every 12 h for 3 days. inhibitory I max model was used PK/PD modeling. Results showed that MIC...

In this study, the Fe-Cr-Ni-Si and WC alloy coatings were deposited on polished 2Cr13 steel samples by using a laser cladding technique. The microstructure, tribology erosion-corrosion resistance properties of investigated, influence proportion analyzed. research results show that ratio in powders affects obviously coatings, when is 20%, coating possesses excellent hardness, wear-resisting erosive-corrosive resistance, which can prolong effectively operating life equipment.

Milbemycin oxime (MBO) and praziquantel (PZQ) have a broad spectrum of biological activity are commonly used to treat the parasitic infection in veterinary clinic. In this study, fast efficient LC-MS/MS method was established validated for simultaneous determination MBO, PZQ, cis-4-hydroxylated-PZQ (C-4-OH-PZQ) trans-4-hydroxylated-PZQ (T-4-OH-PZQ) cat plasma.Extraction analytes internal standards from plasma by acetonitrile protein precipitation, allows rapid processing large batches...

The economic impact of necrotizing enteritis (NE) resulting from Clostridium perfringens infection has been significant within the broiler industry. This study primarily investigated antibacterial efficacy hexahydrocolupulone against C. , and its pharmacokinetics ileal contents chickens. Additionally, a dosing regimen was developed based on pharmacokinetic/pharmacodynamic (PK/PD) model specific to Results indicated that minimum inhibitory concentration (MIC) ranged 2 mg/L 16 in MH broth....

Carbapenem- and colistin-resistant Enterobacter has been a clinical therapy problem in recent years. Here, we report the carbapenem- harboring blaIMI isolated from intestinal samples environment of duck farm China. Four blaIMI-positive isolates were resistant to carbapenem colistin. Three subtypes detected different molecular categories Enterobacter. The detection various IMI producers highlights diversity carbapenemases farm. Whole-genome Sequencing demonstrated genes present chromosomes or...

Abstract Antibiotic resistance is a serious public health crisis. The challenge caused by Staphylococcus aureus infections clearly urges the development of novel antimicrobial therapy. Drug repurposing has emerged as an alternative approach to rapidly identify effective drugs against multidrug-resistant bacteria. Recently, substituted benzene guanidine compounds have been used leading structures discover new promising in both synthetic and medicinal chemistry. We investigated activity analog...

The corrosion behavior of β-Sn and intermetallic compounds in Ag–28Sn alloy was investigated by potentiodynamic polarization bipolar electrochemistry tests. results show that the Na2SO4 solution Ag4Sn preferentially corrode at high potential low potential; NaCl solution, corrodes both potential. To clarify mechanism selective corrosion, an Ag–Sn coupled electrode assembled characterized using test. Based on potential–pH diagram, is elucidated.