methicillin

Methicillin sodium salt is the sodium salt form of methicillin, a semisynthetic beta-lactam penicillin antibiotic with beta-lactamase resistant activity.

Methicillin sodium hydrate, a narrow-spectrum β-lactam antibiotic, inhibits penicillin-binding proteins (PBPs), targeting Staphylococcus aureus and Staphylococcus epidermidis resistant to other penicillins. It is utilized in researching skin infections, osteomyelitis, and endocarditis [1].

Methicillin is a narrow-spectrum beta-lactam antibiotic of the penicillin-like family, used to treat infections caused by susceptible gram-positive bacteria, in particular penicillase-producing organisms such as Staphylococcus aureus.

Oxacillin sodium monohydrate (Stapenor monohydrate) is an antibacterial agent and is a narrow spectrum beta-lactam antibiotic of the penicillin class.

Ceftobiprole (Ro 63-9141) is a broad-spectrum cephalosporin effective against Methicillin-resistant Staphylococcus aureus (MRSA; MIC90: 2 μg mL).

Benzyldodecyldimethylammonium chloride dihydrate can be used as an insecticide reagent. It can target drug-resistant bacteria, such as methicillin-resistant Staphylococcus aureus, multidrug-resistant Pseudomonas aeruginosa, etc., in a concentration-dependent manner.

Linezolid (PNU-100766), the first of the oxazolidinone class, is a synthetic antibiotic used for the therapy of infections resulted from multi-resistant bacteria including methicillin-resistant Staphylococcus aureus (MRSA) and streptococcus. The drug takes effect as the inhibitor of the initiation of bacterial protein synthesis.

Nafcillin sodium monohydrate (CL 8491) is the sodium salt form of nafcillin, a semi-synthetic naphthalene, penicillin-related Nafcillin inhibits bacterial wall synthesis by a mechanism of action similar to penicillin. Penicillinase-resistant Nafcillin is used to treat infections caused by penicillin-resistant strains of Staphylococci.

Dalbavancin (BI-397), a novel second-generation lipoglycopeptide antibiotic, possesses in vitro activity against a variety of Gram-positive pathogens including methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-resistant Staphylococcus epidermidis (MRSE),Dalbavancin inhibits Staphylococcus aureus and Bacillus anthracis with MIC90s of 0.06 μg/mL and 0.25 μg/mL, respectively

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.

(-)-Corynoxidine is an AChE inhibitor derived from tubers of Stephania succifera. Corynoxidine exhibits antibacterial activities against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus strains in different degrees.

Sanguisorbigenin (Tomentosolic acid) is a natural antimicrobial agent that inhibits methicillin-resistant Staphylococcus aureus (MRSA).

Ceftobiprole medocaril (BAL5788), the parenteral prodrug of Ceftobiprole, is a broad-spectrum cephalosporin effective against Methicillin-resistant Staphylococcus aureus (MRSA).

Eperezolid (PNU-100592) is an oxazolidinone antibacterial agent. Eperezolid showed well in vitro inhibitory activity, regardless of methicillin susceptibility for staphylococci(MIC90= 1-4 mg/ml).

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.

Alopecurone A demonstrates potent inhibitory effects on MRP1, exhibits cytotoxic activity against DU145 (prostate cancer cell line) and MCF-7 (breast cancer cell line) with IC50 values of 2.44 and 5.44 μg/mL, respectively, and possesses antibacterial activity against methicillin-resistant Staphylococcus aureus.

Parvodicin C2, a glycopeptide antibiotic derived from A. parvosata and part of the parvodicin complex, serves as a component of the A40926 antibiotic complex utilized as a precursor for synthesizing dalbavancin. It exhibits activity against methicillin-sensitive and methicillin-resistant strains of S. aureus, S. epidermidis, S. saprophyticus, S. hemolyticus, and E. faecalis.

TunR2 is an antibiotic and derivative of tunicamycin .1It is active againstB. subtilis(MIC = 0.3 μg/ml) and increases the efficacy of the β-lactam antibiotics oxacillin , methicillin , and penicillin G againstB. subtiliswhen used at a concentration of 0.4 μg/ml. Unlike tunicamycin, TunR2 is non-toxic toS. cerevisiae(MIC = >10 μg/ml) and does not inhibit glycosylation in a protein N-glycosylation assay. TunR2 also has reduced antiproliferative activity against MDA-MB-231 and CHO cells compared with tunicamycin. 1.Price, N.P., Hartman, T.M., Li, J., et al.Modified tunicamycins with reduced eukaryotic toxicity that enhance the antibacterial activity of β-lactamsJ. Antibiot. (Tokyo)70(11)1070-1077(2017)

Benastatin B is a polyketide synthase-derived benastatin that has been found in Streptomyces and has diverse biological activities. It inhibits glutathione S-transferase (GST; Ki = 3.7 µM for the rat liver enzyme).2 Benastatin B also inhibits the transglycosylase activity of A. baumannii, C. difficile, E. coli, and S. aureus recombinant penicillin-binding proteins (PBPs; IC50s = 16, 53.3, 30.7, and 31.6 µM, respectively).3 It is active against several bacteria, including methicillin-resistant S. aureus (MRSA; MIC = 3.12 µg/ml).

VP-4509 is an anti-methicillin-resistant Staphylococcus aureus (MRSA) agent (MIC: 49.3 μM). VP-4509 exhibits high antibacterial activity against the gram-negative bacterium Pseudomonas aeruginosa (ATCC9027).

BO3482 is an antimicrobial compound and can inhibit the growth of methicillin-resistant Staphylococci (MIC90: 6.25 mg mL).

Laburnetin, an isoflavone antibacterial agent, exhibits antibacterial activity against fungi and S. vesicarium, and enhances the susceptibility of Methicillin-resistant Staphylococcus aureus (MRSA) strains to Methicillin. It is also effective in controlling pests of cultivated species [1] [2] [3].

Anti-MRSA agent 4 (compound 7a), a selective and potent inhibitor of Gram-positive Methicillin-resistant Staphylococcus aureus (MRSA) growth, demonstrates a minimum inhibitory concentration (MIC) of ≤ 0.26 µM and exhibits neither cytotoxic nor hemolytic activity in HEK293 cells [1].

Compound A11 (Antibacterial agent 86) exhibits the highest bacteriostatic activity against methicillin-resistant S. aureus, with minimum inhibitory concentration (MIC) values reaching as low as 0.00191 μg/mL. This efficacy is 162 and 32 times greater than the commercial antibiotics tiamulin and retapamulin, respectively [1].

Antibacterial Agent 136 (Compound 3), an oxadiazolone antibiotic, exhibits high antibacterial potency against Methicillin-resistant Staphylococcus aureus (MRSA), with a minimum inhibitory concentration (MIC) 50 value of 0.8 μM [1].

Pazufloxacin (T-3761) is a fluoroquinolone antibiotic used for antibacterial applications. This novel quinolone derivative exhibits robust and broad-spectrum antibacterial efficacy against systemic, pulmonary, and urinary tract infections in mice, effectively targeting both gram-positive and gram-negative bacteria, including quinolone-resistant strains such as Serratia marcescens and Pseudomonas aeruginosa. Compared to antibiotics like ofloxacin, ciprofloxacin, norfloxacin, and tosufloxacin, Pazufloxacin demonstrates comparable or superior efficacy across various infection models. While slightly less effective than tosufloxacin against certain gram-positive infections, it remains potent against methicillin-resistant Staphylococcus aureus. Its broad-spectrum activity is supported by minimum inhibitory concentrations (MICs) between 0.39 and 6.25 micrograms ml for Staphylococcus aureus and Clostridium species, with minimum bactericidal concentrations (MBCs) close to the MICs. Additionally, its 50% inhibitory concentrations for DNA gyrases from E. coli and P. aeruginosa are 0.88 and 1.9 micrograms ml respectively, highlighting its potent antibacterial mechanism of action.

Anti-MRSA agent 2 (compound 14) is a potent inhibitor of methicillin-resistant Staphylococcus aureus (MRSA) (MIC: 0.098 μg ml), exhibiting relatively low toxicity to normal cells. It strongly disrupts bacterial membranes and effectively binds to bacterial genomic DNA.

Antibacterial agent 98 (compound g37) is an effective oral antibacterial agent that inhibits the ATPase activity of Gyrase B and weakens the DNA super-helix of S. aureus. Notably, it does not induce the development of MRSA (methicillin-resistant Staphylococcus aureus) resistance.

Torachrysone shows promising antioxidant activity. Torachrysone, toralactone , aloe-emodin, rhein and emodin show noticeable antibacterial effects on four strains of methicillin-resistant Staphylococcus aureus with a minimum inhibitory concentration of 2-

Chlorhexidine-d8 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......

CAY10711 is a substituted diamine that produces rapid bactericidal activity against both Gram-positive and Gram-negative bacteria, including methicillin-resistant S. aureus (MRSA) and stationary-phase bacteria. It displays MIC99 values of 2.9, 11.5, 2.9, and 2.9 μM against S. aureus RN4220, P. aeruginosa PAO1, E. coli ANS1, and MRSA 10082B, respectively. CAY10711 reduces biofilm formation and promotes biofilm dispersal in P. aeruginosa. It is synergistic with kanamycin and has limited adverse effects against mammalian cells or C. elegans development, survival, or reproduction.

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

Ceftaroline fosamil hydrate acetate is a powerful cephalosporin antibiotic that exhibits broad-spectrum efficacy against both Gram-positive pathogens, such as methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Streptococcus pneumoniae, and common Gram-negative bacteria. It possesses anti-infective properties suitable for studying complicated skin and skin structure infections (cSSSIs) and community-acquired bacterial pneumonia (CABP) [1] [2] [3].

Pristinamycin, synthesized by Streptomyces pristinaespiralis, is an orally administered antibiotic resembling streptogramin, comprising two distinct components: Pristinamycin I (PI) and Pristinamycin II (PII). This compound exhibits a high efficacy against various antibiotic-resistant pathogens, especially Gram-positive bacteria such as Methicillin-resistant Staphylococcus aureus (MRSA), Vancomycin-resistant S. aureus (VRSA), and Enterococcus faecium (VREF) [1].

Teicoplanin aglycone is an antibacterial glycopeptide antibiotic used in the prophylaxis and treatment of serious infections caused by Gram-positive bacteria, including Enterococcus faecalis and methicillin-resistant Staphylococcus aureus.

TPU-0037C is a metabolite of the marine actinomycete S. platensis that is structurally similar to lydicamycin . It is active against Gram-positive bacteria (MICs = 0.39-3.13 μg/ml), including methicillin-resistant S. aureus strains (MIC = 3.13 μg/ml), but is ineffective against Gram-negative bacteria (MICs = >50 μg/ml).

Anti-MRSA agent 3 inhibits methicillin-resistant Staphylococcus aureus (MRSA) activity significantly (MIC: 0.098 μg/ml) with low toxicity to normal cells. anti-MRSA agent 3 has a high binding affinity for bacterial genomic DNA and a strong ability to disrupt bacterial cell walls and membranes.

PD 117588 is a quinolone against bacterial isolates from cancer patients. PD 117558 has a broad antimicrobial spectrum with excellent activity against all Gram-positive isolates (including methicillin-resistant Staphylococcus aureus, coagulase-negative st

Tedizolid phosphate is a novel antibacterial prodrug. Tedizolid phosphate is a next-generation oxazolidinone with activity against both methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus spp. It also has effective activity a

Parvodicin complex is a mixture of closely related lipophilic glycopeptides originally isolated from A. parvosata. The parvodicin complex has activity against Gram-positive bacteria (MICs = 0.8-12.5 μg/ml) including methicillin-resistant strains of S. aureus (MRSA), S. hemolyticus, and E. faecalis (MICs = 0.1-25 μg/ml). Glycopeptide antibiotics act by preventing cell wall synthesis by binding and sequestering a cell wall precursor with a D-alanine-containing peptide.

DHFR-IN-9 (compound 8A), a dihydrofolate reductase (DHFR) inhibitor, impedes purine and thymidylate biosynthesis, pivotal in cell proliferation and growth. It demonstrates potency against methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 with an IC50 of 0.25 μg/mL and exhibits anti-infective properties in mouse systemic and thigh infection models at doses of 2.5 mg/kg and 5 mg/kg administered intraperitoneally (ip). Furthermore, DHFR-IN-9 shows greater anticancer efficacy in a mouse breast cancer model compared to paclitaxel (Y-B0015), at a regimented dosage of 2.5 mg/kg ip every three days [1].

(E)-3-Hydroxy-5-methoxystilbene possesses inhibitory activity against several Gram-positive bacteria, including isolates of methicillin-resistant Staphylococcus aureus (MRSA), Mycobacterium bovis BCG, and avirulent Bacillusanthracis (Sterne strain), among

3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003). 3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4 References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003).

Ceftobiprole medocaril sodium (BAL5788) is a parenteral prodrug of Ceftobiprole, a pyrrolidinone cephalosporin administered intravenously. As a broad-spectrum cephalosporin, Ceftobiprole exhibits high in vitro activity against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant Staphylococci (VRSA), and penicillin-resistant Streptococci. Additionally, it is effective in inhibiting both gram-positive and gram-negative pathogens.

C16-K-cBB1 is a potent, selective antimicrobial agent effective against Methicillin-resistant Staphylococcus aureus (MRSA), demonstrated by its minimal inhibitory concentration (MIC) of 1 µg/mL. This compound exhibits excellent selectivity with minimal hemolytic activity, and can eradicate MRSA cells within 120 minutes when applied at a concentration of 12.5 μg/mL.

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].

(6E,12E)-Tetradecadiene-8,10-diyne-1,3-diol is an antibacterial compound isolated from the roots of Atractylodes japonica, exhibiting anti-methicillin-resistant Staphylococcus aureus (MRSA) activity with MIC values of 4-32 μg mL, and can be used for the research of bacterial infection [1].

Diallyl tetrasulfide is an organosulfur compound that has been found in A. sativum and has diverse biological activities, including antimicrobial, antioxidant, and anticancer properties.[1],[2],[3],[4] It is active against the bacteria S. aureus and methicillin-resistant S. aureus (MRSA; MICs = 0.5 and 2 mg/L, respectively), as well as the fungi C. albicans, C. krusei, C. glabrata, A. niger, A. flavus, and A. fumigatus (MICs = 0.5, 4, 2, 1, 2, and 4 mg/L, respectively).[1] It reduces cadmium-induced increases in hepatic levels of thiobarbituric acid reactive substances (TBARS) and increases cadmium-induced decreases in the hepatic activity of superoxide dismutase (SOD1), catalase, GST, and glucose-6-phosphate dehydrogenase (G6PDH) in rats when administered at a dose of 40 mg/kg.[2] Diallyl tetrasulfide is cytotoxic to MCF-7 breast cancer cells (IC50 = 92 μM) and reduces tumor growth in a BGC-823 mouse xenograft model when administered at doses of 20, 30, and 40 mg/kg for 32 days.[3],[4]

VP-4604 is a potent anti-methicillin-resistant Staphylococcus aureus (MRSA) compound that exhibited significant microbial growth inhibition against S. aureus with an MIC of 4-8 μg mL and a growth inhibition rate of over 95%.

6-Methoxydihydrosanguinarine is a natural product. 6-Methoxydihydrosanguinarine shows strong cytotoxicity against MCF-7 and SF-268 cell lines with IC50 values of 0.61 μM and 0.54 μM, respectively.It has antibacterial activity against Methicillin-resistant Staphylococcus aureus (MRSA) strains with minimum inhibitory concentrations (MICs) ranging from1.9 to 3.9 microg ml

Chlorhexidine (Rotersept) is a biguanide compound used as an antiseptic agent with topical antibacterial activity. Chlorhexidine is positively charged and reacts with the negatively charged microbial cell surface, thereby destroying the integrity of the cell membrane. Subsequently, chlorhexidine penetrates into the cell and causes leakage of intracellular components leading to cell death. Since gram-positive bacteria are more negatively charged, they are more sensitive to this agent.

Chlorhexidine dihydrochloride (NSC-185) is a disinfectant and topical anti-infective agent used also as mouthwash to prevent oral plaque.

Chlorhexidine digluconate is a broad-spectrum antiseptic and disinfectant with broad-spectrum antimicrobial activity, inhibits both Gram-positive and Gram-negative bacteria, induces necrosis and apoptosis, and can be used in the study of bacterial infections.

Chlorhexidine diacetate (Bactigras) is a disinfectant and topical anti-infective agent used also as mouthwash to prevent oral plaque.