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.

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.

Galegine hydrochloride, a guanidine derivative derived from G. officinalis, plays a role in inducing weight loss in mice and has contributed to the development of biguanides, including metformin and phenformin. This compound stimulates AMPK activation in 3T3-L1 adipocytes, L6 myotubes, H4IIE rat hepatoma, and HEK293 human kidney cell lines. Additionally, galegine hydrochloride exhibits antibacterial properties, particularly demonstrating a minimum inhibitory concentration of 4 mg L against Staphylococcus aureus strains[1][2].

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg/ml) and Gram-negative bacteria (MICs = 136-200 µg/ml), as well as yeasts (MICs = 10-20 µg/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces tumor growth in a B16/BL6 mouse model of melanoma when administered at a dose of 25 mg/kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg/kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 µg/ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg/kg.3Ajoene (25 mg/kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16/BL6 melanoma cells in C57BL/6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)

Bismuth subcarbonate, also known as bismuth carbonate oxide, is a versatile semiconductor compound based on bismuth, commonly utilized for its antibacterial properties, as well as in various applications such as sensors, super capacitors, and photocatalysts. Additionally, bismuth subcarbonate serves as a protective agent against gastric acid erosion, particularly in the treatment of gastric ulcers[1][2].

2,6-Dimethylbenzoquinone (2,6-Dimethylquinone) is a benzoquinone, a chemical compound found in Rauvolfia vomitoria and in Tibouchina pulchra.At physiological concentrations 2, 6-Dimethoxy-p-benzoquinone is an antibacterial substance

1. Artemisic acid ((+)-Artemisinic Acid) shows antibacterial activity. 2. Artemisinic acid is a major precursor of artemisinin (an antimalaric compound), isolated as the active principles of the medicinal plant Artemisia annua L.

2-[(2S,5S)-5-(carbamoylmethyl)-3,6-dioxopiperazin-2-yl]acetamide is a compound used as a molecular structural unit, a cyclic dipeptide. It induces apoptosis, inhibits cell proliferation and modulates immune responses, and possesses a wide range of biological activities including antitumor, antifungal, antibacterial, antiviral and immune-conditioning activities.

MurA-IN-2 (compound 37), a potent MurA inhibitor featuring a chloroacetamide fragment with a primary aliphatic amine, exhibits antibacterial activity by inhibiting bacterial cell wall synthesis, with an IC50 of 39 μM [1].

Metallo-β-lactamase-IN-8 (compound 17) is a potent, reversible, and competitive broad-spectrum metallo-β-lactamases (MβLs) inhibitor with antibacterial activity, exhibiting IC50 values of 1.3 μM against L1, 5.7 μM against ImiS, 9.8 μM against IMP-1, and 9.9 μM against VIM-2 [1].

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].

Sulfisoxazole diethanolamine, also known as Sulfafurazole diethanolamine, is a sulfonamide antibacterial compound with an oxazole substituent. It acts as an endothelin receptor antagonist, specifically targeting endothelin receptor A with an IC50 value of 0.60 μM and endothelin receptor B with an IC50 value of 22 μM. Additionally, Sulfisoxazole diethanolamine has been found to inhibit the release of breast cancer exosomes by specifically targeting endothelin receptor A [1] [2].

MtTMPK-IN-4 (compound 2), a para-piperidine, is a highly potent inhibitor of thymidylate kinase (MtTMPK) in Mycobacterium tuberculosis with an IC50 value of 6.1 μM, and exhibits remarkable tyrosinase inhibitory activity and potent antibacterial properties [1] [2].

MraY-IN-2 (compound 6) is a potent inhibitor of bacterial transposase MraY (IC50=4.5 μM), suitable for antibacterial research.

14α-Demethylase DNA Gyrase-IN-2 (Compound 6a) is a potent inhibitor of 14α-Demethylase and DNA Gyrase, exhibiting significant antibacterial activity.

VIM-2-IN-1 (compound 1dj) is a β-lactamase inhibitor with antibacterial activity, demonstrating an IC50 of 48 μM, and inhibits New Delhi Metal (NDM-1) with an IC50 of 231 μM.