Antibacterial compound 2

Antibacterial compound 2 is a potent antimicrobial agent effective against many human veterinary pathogens, inhibiting multi-drug resistant staphylococci, enterococci and streptococci, as well as anaerobic bacteria.

2-Hydroxypalmitic acid is a saturated long-chain 2-hydroxy fatty acid with potential anti-inflammatory, antibacterial, anticancer, and neuroprotective activities, and it can also function as a surfactant.

Thiocillin I, a thiopeptide antibiotic, demonstrates potent in vitro antibacterial effects against Gram-positive bacteria. This compound exhibits minimum inhibitory concentrations (MICs) of 2 μg/mL, 0.5 μg/mL, 4 μg/mL, and 0.5 μg/mL against S. aureus 1974149, E. faecalis 1674621, B. subtilis ATCC 6633, and S. pyogenes 1744264, respectively.

AVX 13616, Avexa's leading antibacterial candidate, demonstrates significant in vivo antibacterial efficacy, especially against drug-resistant Staphylococcus pathogens, with an IC50 value of 2-4 µg/ml (MICs) and is targeted as an antibacterial agent. Comparable in activity to mupirocin within a nasal decolonization model, AVX13616 necessitated only a single application for effectiveness. This compound, alongside others, exhibited broad-spectrum antibacterial action, achieving MICs of 2-4 micrograms per milliliter against various isolates, including S. aureus, coagulase-negative staphylococci, enterococci, MRSA, VISA, and VRSA. Aimed for topical use and the treatment of wound infection or catheter-related infections, a solitary 5% (w/w) AVX13616 application (roughly equivalent to 2% mupirocin) proved as efficacious as twice-daily 2% mupirocin over five days in decolonizing MRSA in mice.

Ppc-1 is a chemical compound known for its inhibitory effects on the Gram-negative periodontopathogen Porphyromonas gingivalis. It acts as a mitochondrial uncoupler, enhancing mitochondrial oxygen consumption without affecting ATP production. Additionally, Ppc-1 serves as a cell-permeate inhibitor of interleukin-2 (IL-2). This compound exhibits various beneficial activities, including anti-obesity, antibacterial, and anti-inflammatory properties.

Amifloxacin (Win49375) is a synthetic antibacterial compound demonstrating moderate activity against Staphylococcus aureus, with MICs ≤ 2 micrograms/ml.

Apoptosisinducer 26 (compound [AgCl(dap2SH)(PPh3)2]) is a mononuclear Ag(I) ligand-based autophagy inducer that exhibits antibacterial and anticancer activities against various bacterial strains and cancer cell lines. This compound facilitates the accumulation of Ag(I) ions in the periphery of bacteria, effectively inhibiting the growth of both Gram-positive (+) and Gram-negative (-) bacteria. Additionally, Apoptosisinducer 26 can intercalate between the base pairs of CT DNA, inducing apoptosis in A549 cells. It also possesses radical scavenging properties, which helps prevent oxidative stress.

Antibacterialagent 255 (compound (±)-1) is a potent antibacterial agent, acting as an effective and selective inhibitor of 4-diphosphocytidyl-2-C-methyl-D-erythritol (IspE). It exhibits IC50 values of 13.0, 8.0, and 20 µM against EclspE, KplspE, and AblspE, respectively.

Antimicrobial agent-35 (Compound c9) demonstrates antibacterial activity, effectively inhibiting S. aureus, E. coli, E. faecalis, and S. maltophilia with a MIC of 0.5-2 μg/mL. Additionally, Antimicrobial agent-35 shows cytotoxicity towards HT-22 cells, with an IC50 value of 130.4 μg/mL.

Anti-neuroinflammation agent 2 (compound 4) exhibits both anti-neuroinflammatory and antibacterial properties, with an IC50 value of 3.06 µM for TNF-α, an IC50 value of 4.31 µM for IL-6, and an EC50 value range of 0.87 to 3.16 µM for Gram-positive bacteria.

ROS inducer 8 (Compound 11g) acts as an inhibitor of glutathione (GSH) and promotes the accumulation of reactive oxygen species (ROS) in Enterococcus faecalis, exhibiting antibacterial properties. It is capable of disrupting biofilms and inhibiting S. aureus and E. faecalis with minimum inhibitory concentrations (MICs) of 8 μg/mL and 2 μg/mL, respectively, demonstrating a post-antibiotic effect. Additionally, ROS inducer 8 shows low hemolytic toxicity on sheep red blood cells with an HC50 greater than 1280 μg/mL.

Antibacterialagent 272 (Compound Z22) is a potential antibacterial agent that targets the DNA and DNA-topoisomerase II (DNA-Topo II) complex. It exhibits strong antibacterial activity, with a minimum inhibitory concentration (MIC) of 1 μg/mL against Staphylococcus aureus 25923 and 29213, 2 μg/mL against Staphylococcus epidermidis 12228, 2-4 μg/mL against Enterococcus faecalis, and 4 μg/mL against Pseudomonas aeruginosa 9027 and 27853. Antibacterialagent 272 binds by intercalating between DNA base pairs, disrupting the normal function of bacterial DNA, and is suitable for research into bacterial infectious diseases.

FtsZ-IN-13 (Compound C11) functions as an inhibitor of the temperature-sensitive mutant Z (FtsZ), exhibiting IC50 values of 47.97 μM for FtsZSa and 34 μM for FtsZPa. It demonstrates notable antibacterial activity against Staphylococcus aureus (with a minimum inhibitory concentration of 2 μg/mL), cystic fibrosis Staphylococcus aureus clinical isolates, and methicillin-resistant Staphylococcus aureus (MRSA). FtsZ-IN-13 is applicable in research on antibiotic resistance.

Florfenicol-propanoate-piperidin (Compound 1) is a derivative of Florfenicol. This compound exhibits antibacterial activity, effectively inhibiting strains such as E. coli ATCC25922, Salmonella CICC110420, S. aureus ATCC29213, B. subtilis CMCC(B)63501, E. faecalis ATCC29212, S. suis CVCC606, and Haemophilus parasuis, with a minimum inhibitory concentration (MIC) ranging from 2 to 8 μM.

PD-L1/LpxC-IN-1 (Compound 12b) is an inhibitor of PD-L1 and LpxC, with IC50 values of 5.2 μM and 0.081 μM, respectively. This compound disrupts bacterial lipopolysaccharide biosynthesis, leading to bacterial cell lysis and death. It effectively inhibits Gram-negative bacteria, exhibiting a minimum inhibitory concentration (MIC) of 0.25-0.5 μg/mL against K. pneumoniae ATCC 13883, E. coli ATCC 8739, S. typhimurium ATCC 14028, and P. aeruginosa ATCC 9027. Additionally, PD-L1/LpxC-IN-1 modulates the immune response by downregulating the expression of inflammatory cytokines IL-2 and IFN-γ, and upregulating CD4+ and CD8+ cells, thus activating the immune system and mitigating excessive inflammatory responses. In a mouse model of K. pneumoniae ATCC 13883 infection, PD-L1/LpxC-IN-1 demonstrated antibacterial activity.

Antibiofilm agent-8 (compound Ru2) boosts antibacterial activity under visible light (400-700 nm, 10 J cm-2). It induces oxidative stress by promoting NADH oxidation and reactive oxygen species (ROS) generation, which disrupts the bacterial cell wall.

Antimicrobial agent-32 (Compound 4g) is an antibacterial compound with significant efficacy against several bacteria, including Staphylococcus aureus, Bacillus subtilis, Bacillus cereus [MIC=1000 µg/mL], Klebsiella pneumonia, and methicillin-resistant Staphylococcus aureus [MRSA] [MIC=500 µg/mL], as well as Escherichia coli [MIC=250 µg/mL]. Additionally, Antimicrobial agent-32 exhibits anticancer activity by inhibiting the proliferation of MCF-7, HCT-116, and HepG-2 cells.

Antibacterialagent 226 (Compound 7f) is an antibacterial agent effective against Staphylococcus aureus strains, including methicillin-resistant S. aureus, with a MIC of 2 μg/mL. It exhibits cytotoxicity towards HEK293 cells with an IC50 of 1.9 μM.

Antibacterial agent 228 (Compound 8) inhibits mycobacterial ribosomes with an IC50 of 2.31 μM against Mycobacterium smegmatis. It demonstrates antibacterial activity with MIC values of 2 and 0.25 μg/mL against both wild-type and Δ1258c mutant strains of M. tuberculosis H37Rv, 8 μg/mL against wild-type and Δ2780c mutant strains of M. abscessus ATCC 19977, and 8 μg/mL against M. smegmatis.

SARS-CoV-2 Mpro-IN-21 (compound A8) is an effective inhibitor of the SARS-CoV-2 and COVID-19 Main Protease MPro. It demonstrates significant antioxidant activity in the DPPH assay with an IC50 of 0.36 mg/mL. SARS-CoV-2 Mpro-IN-21 also shows notable antibacterial activity against Klebsiella, with an IC50 of 1.19 mg/mL.

Anti-MRSA agent 14 (Compound C17) exhibits antibacterial activity against MRSA and in a MRSA-infected mouse skin model. It demonstrates greater potential against MRSA compared to Norfloxacin. Anti-MRSA agent 14 disrupts cell membranes and inhibits metabolism. Its antibacterial MIC values against S. aureus ATCC 6538, S. aureus ATCC 29213, S. epidermidis ATCC 12228, and MRSA are 1, 2, 2, and 1 μM, respectively.

Antibacterialagent 285 (Compound 3) is a cephalosporin antibiotic. It exhibits significant antibacterial activity against Gram-negative bacteria, with minimum inhibitory concentrations (MIC) of 0.125-0.5 μg/mL for carbapenem-resistant Acinetobacter baumannii (CRAB), 0.125-0.5 μg/mL for Klebsiella pneumoniae (CRE), and 0.125-2 μg/mL for Pseudomonas aeruginosa (CRPA). Antibacterialagent 285 can be utilized in bacterial infection research, including studies on complicated urinary tract infections (cUTI) and kidney infections.

KPC-2-IN-3 (Compound 3b) is a KPC-2 inhibitor with an IC50 of 0.533 μM and a Ki of 0.194 μM. It works synergistically with Meropenem to exhibit antibacterial activity against carbapenem-resistant K. pneumoniae K47-25, reducing bacterial count and demonstrating a post-antibiotic effect. Additionally, KPC-2-IN-3 significantly decreases lung bacterial load in a mouse pneumonia model.

DNA gyrase/Topo IV-IN-2 (Compound AK19) is an antibacterial agent with IC50 values of 0.783 μM and 7.136 μM for inhibiting E. coli DNA gyrase and topoisomerase IV, respectively. It exhibits broad-spectrum antibacterial activity against both Gram-positive and Gram-negative pathogens and inhibits biofilm formation in B. subtilis and MRSA, with a MIC of 1.9 μM. DNA gyrase/Topo IV-IN-2 is useful for researching drugs targeting resistant bacteria.