Antibacterial

4-Aminosalicylic acid hemicalcium, an orally active antibiotic, shows potential in tuberculosis research [1].

Sterculic acid methyl ester, an ester derivative of sterculic acid known for inhibiting Δ9 desaturase, has been found to adversely affect and exhibit toxicity towards R. opacus bacteria at a concentration of 0.75 mM. It not only hampers bacterial growth but also modifies fatty acid composition by reducing stearate and oleate levels, increasing the palmitate ratio, and decreasing overall fatty acid content at 0.25 or 0.5 mM concentrations. Additionally, at 50 ppm, Sterculic acid methyl ester enhances the tumor growth-promoting effects of aflatoxin Q1 in rainbow trout, indicating a synergistic interaction between the two compounds. [Matreya, LLC. Catalog No. 1236]

TH-Z145 is a potent FPPS inhibitor for the study of myeloma and lung cancer.

Tylvalosin (Acetylisovaleryltylosin) is a broad-spectrum macrolide antibiotic with antibacterial and antiviral properties, effective against PRRSV infection.

4-Nitrophenyl palmitate serves as a colorimetric substrate for lipase and esterase, enabling the quantification of enzyme activity through the release and colorimetric detection of 4-nitrophenol at 410 nm following enzymatic hydrolysis. This compound facilitates the characterization of enzyme activity across diverse bacterial and mammalian sources, including Burkholderia and porcine pancreatic lipases.

TP0480066 inhibits topoisomerase II, DNA gyrase (IC50=1.1nM), topo IV (IC50=62.89nM), effective against drug-resistant bacteria and N. gonorrhoeae.

Trovafloxacin: broad-spectrum fluoroquinolone, blocks DNA gyrase/topoisomerase IV and PANX1 channel (IC50=4μM).

Deoxynybomycin, a selective anti-tumor agent, inhibits topoisomerase I and induces apoptosis.

Variculanol, a compound with antimicrobial, anticancer, and anti-HCV NS3/4A protease properties, is derived from the marine fungus Aspergillus versicolor [1].

DprE1-IN-9 (compound B18) is an efficient reversible inhibitor of DprE1, interacting with the enzyme's receptor cavity.

AU1235 is a Mycobacterium tuberculosis inhibitor.

Tuberculosis inhibitor 6 (compound 2c), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, is highly active against Mycobacterium tuberculosis (MIC 90 of

MurA-IN-4 exhibits antibacterial properties as a MurA inhibitor, impeding the synthesis of bacterial cell walls [1].

DQn-1, a potent antifolate, demonstrates efficacy against Mycobacterium tuberculosis (Mtb) with an MIC 90 of 0.03 µM.

Avarol triggers cell death in pancreatic cancer and is a non-toxic, neuroprotective AChE inhibitor for Alzheimer's.

Pristinamycin IA (Mikamycin B) is a substrate for the P-glycoprotein and a cyclo-peptidic macrolactone antibiotic.

Antibacterial compound 2 is a potent antimicrobial agent effective against many human veterinary pathogens, inhibiting multi-drug resistant staphylococci,

Pexiganan acetate (MSI 78), a 22-residue peptide analogue of magainin 2, disrupts bacterial membranes or walls, leading to antibacterial activity.

Antibiofilm agent-9 (Compound 4), a derivative of pyrrolnitrin, exhibits antimicrobial activity. It inhibits Bacillus anthracis with a Minimum Inhibitory Concentration (MIC) of 0.031 μg/mL. The compound demonstrates significant antibiofilm activity, achieving an inhibition rate of 84% after 24 hours at a concentration of 8.0 μg/mL. Additionally, Antibiofilm agent-9 shows favorable pharmacokinetic properties in mouse models.

Acorafloxacin: broad-spectrum fluoroquinolone antibacterial for acute skin infections and pneumonia.

Frenolicin is a selective inhibitor of Prx1 and Grx3 through covalent modification of active-site cysteines.

Bassianolide, a cyclodepsipeptide insecticide produced by the fungal species B. bassiana and V. lecanii, demonstrates significant biological activity. Upon oral administration, it induces atony in B. mori silkworms at a concentration of 4 ppm and becomes lethal when concentrations exceed 8 ppm. Remarkably, atony in silkworm larvae can also be triggered by doses as low as 2 µg/larva. Further studies reveal that bassianolide (0.01-1 µM) specifically targets muscarinic receptors to inhibit contractions in isolated guinea pig smooth muscle tissue, elicited by acetylcholine, without affecting nicotinic receptor-induced contractions.

4-Aminobenzylphosphonic acid, an inhibitor of alkaline phosphatase (Ki= 1.1 mM for the bovine intestine enzyme), is utilized in affinity chromatography for alkaline phosphatase purification and in the electrochemical modification of glassy carbon electrodes.

DNA Gyrase-IN-8 is a potent inhibitor of DNA gyrase, demonstrating antimicrobial activity with an IC50 of 8.45 µM [1].

ThrRS-IN-3: Potent inhibitor of Salmonella enterica ThrRS, IC50 = 19 nM, Kd = 34 nM, with antibacterial effects.

Urease Inhibitor 07 is an isosubstituted metalloproteinase inhibitor with potential activity against Mycobacterium tuberculosis strain H37Rv.

Antibacterial Agent 154 (Compound 7), a Fluoroquinolone derivative, exhibits broad-spectrum efficacy against both Gram-positive and Gram-negative bacteria when

L-Methioninamide hydrochloride is a potent inhibitor of methionyl-tRNA synthetase that reduces the toxicity of CDDP.

Elastase LasB-IN-1 (Compound 4b), a potent and selective inhibitor of elastase LasB, exhibits antibacterial activity and has been determined to possess an IC50

Micronomicin (Gentamicin C2b) is an antibiotic exhibiting antibacterial and bactericidal capacity.

TMV-IN-2, a chalcone, inhibits TMV with an EC50 of 89.9 μg/mL, used in infection and tumor studies.

Ganfeborole HCl (GSK3036656 HCl) is a compound with anti-tuberculosis activity and is an inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase.

Pradofloxacin is a fluoroquinolone antibioticthat exerts its bactericidal effect by inhibiting bacterial DNA gyrase and topoisomerase IV.

SA09-Cu is a potent, noncompetitive inhibitor of NDM-1, with an IC50 of 9.6 nM.

IpOHA is a potent inhibitor of plant KARI and functions as an antimycobacterial agent, demonstrating a K_i value of 97.7 nM against Mycobacterium tuberculosis (

β-Lactamase-IN-2 is an inhibitor of β-Lactamase with anti-microbial and anti-bacterial effects.

Tuberculosis inhibitor 7 (compound 2d), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, exhibits potent activity against Mycobacterium tuberculosis and

Vaborbactam (RPX7009) is a β-lactamase inhibitor that is often used in conjunction with meropenem to study pneumonia and CRE infections.

NSC309401 is an E. coli dihydrofolate reductase inhibitor, displaying potency with an IC50 value of 189 nM and a dissociation constant (KD) of 14.57 nM [1].

G43-C3-TEG is a glycosyl-transferase inhibitor that diminishes biofilm formation by inhibiting the synthesis of extracellular polysaccharides (EPS) [1].

LY 173013 is a bicyclic pyrazolidinone, it has antibacterial properties.

Ianthelliformisamine B TFA, an antibiotic enhancer, is used to against resistant Gram-negative bacteria.

Quorum Sensing-IN-2 (compound 23e) is a quorum sensing inhibitor that curtails bacterial pathogenicity without impeding growth.

BAY-Y 3118, a new chlorofluoroquinolone, has antimicrobial activity.

Antibacterial 91: Inhibits aaRS, IC50 2.10μM vs. S. enterica ThrRS, has antibacterial properties. [1]

A 33853 is an antibiotic isolated from culture broth of Streptomyces sp.

Peptide 46 is a short peptide that inhibits SC-dependent DNA synthesis by targeting the bacterial sliding clamp (SC).

L 680833 is an orally active monocyclic beta-lactam human polymorphonuclear leukocyte elastase inhibitor.

Biotin-cholesterol, a biotinylated derivative of cholesterol, serves as a precursor in the manufacturing of biotin-conjugated liposomes and micelles, which are utilized in drug delivery systems [1].