mssa

PK150 shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations.

Delpazolid (LCB01-0371), also known as LCB01-0371, is a new oxazolidinone with cyclic amidrazone. In vitro activity of LCB01-0371 against 624 clinical isolates was evaluated and compared with those of linezolid, vancomycin, and other antibiotics. LCB01-0371 showed good activity against Gram-positive pathogens. In vivo activity of LCB01-0371 against systemic infections in mice was also evaluated. LCB01-0371 was more active than linezolid against these systemic infections. LCB01-0371 showed bacteriostatic activity against Staphylococcus aureus.

Targocil is used as a bacteriostatic inhibitor of wall teichoic acid (WTA) biosynthesis which can inhibit the growth of methicillin-susceptible S. aureus (MSSA) and methicillin-resistant S. aureus (MRSA) (MIC90s: 2 μg/ mL) for both MRSA and MSSA.

Glycosyltransferase-IN-1 is a glycosyltransferase inhibitor with bacteriostatic activity, inhibiting MSSA, MRSA, Bacillus subtilis, and Enterobacteriaceae.

Povidone iodine (Povidone-iodine) exhibits superior antibacterial properties, effectively targeting both MRSA and MSSA strains with minimum inhibitory concentrations (MICs) of 31.25 mg/L and 7.82 mg/L, respectively.

Biotin protein ligase-IN-1 (Compound Bio-9) is an inhibitor of biotin protein ligase (BPL) with a Kd of 7 nM. This compound exhibits antimicrobial activity, with minimum inhibitory concentration (MIC) values of 0.2 μM against Staphylococcus aureus (including MRSA and MSSA) and 20 μM against Mycobacterium tuberculosis.

Anti-MRSA agent 26 (compound 21) is an antibiotic that serves as a potent MRSA inhibitor. It exhibits a MIC of <0.015 μg/mL for MSSA and a MIC range of 0.015-0.06 μg/mL for MSSA, MRSE, and VRE. In a murine model of Staphylococcus aureus skin infection, Anti-MRSA agent 26 effectively clears the infection. It is a 7-deazapurine pyridine with potential application for treating topical infections caused by multidrug-resistant Gram-positive bacteria.

MAO-A/B-IN-4 is an orally active inhibitor of MAO-A/B with IC50 values of 51.3 μM and 47.0 μM, respectively. It demonstrates potent activity against S. aureus, MSSA, MRSA, LRSA, and LREFa. In a mouse model of LRSA peritonitis infection, MAO-A/B-IN-4 shows significant antibacterial efficacy. It is applicable for research into bacterial infections.

(-)-Viriditoxin is a mycotoxin originally isolated from A. viridinutans that has antibacterial and antiproliferative activity. It is active against methicillin-sensitive and -resistant S. aureus (MSSA and MRSA, respectively), tetracycline-sensitive and -resistant Staphylococcus, vancomycin-sensitive and -resistant Enterococcus, and penicillin-sensitive and -resistant S. pneumoniae (MICs = 2-32 μg/ml). (-)-Viriditoxin is also active against fish pathogens, including S. iniae and S. parauberis (MICs = 0.16-0.21 μg/ml). It inhibits polymerization and the GTPase activity of E. coli FtsZ, a tubulin-like GTPase involved in bacterial cell division (IC50s = 8.2 and 7 μg/ml, respectively). (-)-Viriditoxin inhibits proliferation of human DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5.36, 0.63, and 7.6 μM, respectively) . It is also toxic to mice (LD50 = 2.8 mg/kg, i.p.).

VEGFR-2/DHFR-IN-1 (compound 8b) is a chemical inhibitor of VEGFR-2 and DHFR, with IC50 values of 0.384 μM and 7.881 μM, respectively. It possesses effective antibacterial activity against pathogens including Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA, and MRSA, with MIC values ranging from 8 to 16 μg/mL. Additionally, it exhibits potent cytotoxicity against cancer cell lines C26, HepG2, and MCF7, with IC50 values between 2.97 and 7.12 μM, making it a valuable tool for cancer research [1].

FtsZ-IN-2 is an inhibitor of the bacterial cytokinin FtsZ and has an inhibitory effect on GTPase activity. ftsZ-IN-2 exhibited anti-staphylococcal effects with MIC values of 2 μg/ml for both MSSA and MRSA.

Chlorhexidine-D8 hydrochloride is intended for use as an internal standard for the quantification of chlorhexidine by GC- or LC-MS. Chlorhexidine is a bis (biguanide) antimicrobial disinfectant and antiseptic agent. It inhibits growth of clinical methicillin-resistant S. aureus (MRSA) isolates (MIC90 = 4 μg/ml). It is also active against canine isolates of MRSA, methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. pseudintermedius (MRSP), and methicillin-susceptible S. pseudintermedius (MSSP; MIC90s = 4, 2, 2, and 1 mg/L, respectively). Chlorhexidine inhibits growth of E. faecium strains (MICs = 1.2-19.6 μg/ml) and C. albicans (MIC = 5.15 μg/ml). It generates cations that bind to and destabilize the bacterial cell wall to induce death.6 Chlorhexidine also completely inhibits matrix metalloproteinase-2 (MMP-2) and MMP-9 when used at concentrations of 0.0001 and 0.002%, respectively, in a gelatin degradation assay. Formulations containing chlorhexidine have been used in antisept......

Glicophenone, an antibacterial agent, demonstrates minimum inhibitory concentrations (MICs) of 32 μg/mL against multiple strains, including MRSA OM481, MRSA OM505, MRSA OM584, MRSA OM623, and MSSA 209P [1].

Levonadifloxacin ((S)-(-)-Nadifloxacin; WCK 771), a broad-spectrum anti-staphylococcal agent, exhibits antibacterial activity against both Methicillin-susceptible Staphylococcus aureus (MSSA) and Methicillin-resistant S. aureus (MRSA) strains, effectively reducing these bacteria when phagocytosed by THP-1 monocytes [1].

Garvicin KS (GarKS) is a bacteriocin composed of a 34 amino acid peptide, GakA, and two additional peptides, GakB and GakC. GakA alone has been found to reduce fibroblast viability and proliferation. When combined with GakB, GakA forms an effective duo that exhibits notable peptide stability, antimicrobial potency, and an influence on fibroblast viability and proliferation. Among the Garvicin KS peptides, GakB is the most effective against MSSA, with minimum inhibitory concentration (MIC) values ranked as GakB > GakC > GakA [1].

Garvicin KS (GarKS) is a bacteriocin comprising a 34-amino-acid peptide, GakB, along with two additional peptides, GakA and GakC. GakB specifically impairs fibroblast viability and proliferation. When combined with GakA, GarKS demonstrates enhanced peptide stability, antimicrobial activity, and notable impacts on fibroblast viability and proliferation. Regarding methicillin-sensitive Staphylococcus aureus (MSSA) inhibition, minimum inhibitory concentration (MIC) values rank the peptides in descending order of effectiveness as GakB, followed by GakC, and then GakA [1].

Garvicin KS is a 32-amino-acid peptide that, in collaboration with two other peptides, GakA and GakB, constitutes the bacteriocin GarKS. This compound impairs fibroblast viability and proliferation and exhibits antimicrobial activity against MSSA, demonstrating minimum inhibitory concentration (MIC) values ranked as GakB > GakC > GakA [1].

Levonadifloxacin arginine ((S)-(-)-Nadifloxacin; WCK 771) is a broad-spectrum anti-staphylococcal agent. It exhibits antibacterial activity against both methicillin-susceptible Staphylococcus aureus (MSSA) and methicillin-resistant Staphylococcus aureus. Additionally, it reduces monocyte THP-1 phagocytosis of MRSA and MSSA strains.

GW779439X is a pyrazolopyridazine compound that inhibits the S. aureus kinase Stk1 and Aurora kinase A (AURKA). It restores the efficacy of β-lactam antibiotics against methicillin-resistant (MRSA) and methicillin-susceptible (MSSA) S. aureus, often re-sensitizing resistant strains. This antibacterial potentiation is achieved through the induction of apoptosis via caspase-3/7 pathway activation.

Continentalic acid from Aralia continentalis exhibits minimum inhibitory concentrations (MICs) of approximately 8-16 µg/mL against S. aureus, including Methicillin-resistant Staphylococcus aureus (MRSA), Methicillin-susceptible Staphylococcus aureus (MSSA), and standard strains.

Artanin displays promising inhibition against both MSSA and MRSA with minimal inhibitory concentrations (MICs) of 8-64 ug/ml, but very weak against Gram-negative pathogen and yeast with MICs of 256 to ≥1024 ug/ml.

Picrasidine S shows the potent cytotoxicity against human HeLa cervical, gastric MKN-28, and mouse melanoma B-16 cancer cells, it also shows the potent antibacterial activity against two strains of pathogenic bacteria methicillin-resistant Staphylococcus