Antibacterial

JPL is an InhA-cofactor-ligand 3FNG inhibitor and is used for the study of tuberculosis [1].

Compound 6q, a trifluoromethylpyridine oxadiazole, targets Xanthomonas oryzae with EC50 of 7.2 μg/mL.

MsbA-IN-3 is a potent and highly selective MsbA inhibitor (IC50: 2 nM). MsbA-IN-3 inhibits Escherichia coli activity (MIC: 35 μM).

Urease-IN-16, with an IC50 of 132 µmol/L, is a urease inhibitor that coordinates with nickel atoms through the oxygen atoms of either carbonyl or boronic acid groups. This compound holds significant potential as an additive in the development of efficient fertilizers and medical applications.

Meclocycline: a tetracycline antibiotic, inhibits LDH, reduces cell toxicity from mutant huntingtin, doesn't change protein levels in PC12 cells.

PROTACeDHFR Degrader-2 (compound 7b) is an effective degrader targeting Escherichia coli dihydrofolate reductase (eDHFR), capable of reliably degrading eDHFR-tagged proteins.

Altersolanol A (Stemphylin; NSC 173943) demonstrates effective antimicrobial properties, inhibiting the growth of Bacillus subtilis and Pseudomonas aeruginosa with a minimum inhibitory concentration (MIC) ranging from 25-100 μg/mL. Additionally, it shows no phytotoxic effects on Taxus at a concentration of 4 μg/μL.

AK-968-11563024 is an inhibitor targeting marine V. vulnificus NAT [(VIBVN)NAT] with an IC50 value of 18.86 µM. In V. vulnificus, NAT (aromatic amine N-acetyltransferase) plays a role in drug metabolism, contributing to drug resistance. Thus, AK-968-11563024 can be used for research related to drug tolerance.

Glutamate-5-kinase-IN-1 is a potent G5K inhibitor with a 4.1 μM MIC, showing promise in anti-TB research.

Dioxidine is an antimicrobial agent that can inhibit bacterial growth. It is utilized in research on pyogenic infections.

10(R)-hydroxy Stearic acid is a hydroxy fatty acid resulting from the hydroxylation of oleic acid, produced by gut microbiota.

Lavendomycin can be extracted from Streptomyces lavendulae and has active against Gram-positive bacteria.

Vitamin K5 (hydrochloride), a naphthoquinone compound, exhibits trichomonacidal activity in vitro and can be utilized for anti-infection research [1].

MtTMPK-IN-5 inhibits Mtb TMPK with IC50 of 34 μM and fights tuberculosis with MIC of 12.5 μM, aiding TB research.

4-Hexen-3-one inhibits the growth of H. pylori in the ATCC 43526 strain and TDR strain. Additionally, this compound suppresses urease activity.

Carbonic anhydrase inhibitor28 (Compound 11) serves as an inhibitor for the Pseudomonas aeruginosa carbonic anhydrase. It exhibits antibacterial activity, with minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values of 0.5 and 1 μg/mL, respectively, against P. aeruginosa. Carbonic anhydrase inhibitor28 is utilized in research focused on anti-infection applications.

MetRS-IN-1 (Compound 27) is an inhibitor of E. coli methionyl-tRNA synthetase (MetRS) with an IC50 value of 237 nM [1].

9-tert-Butyldoxycycline exhibits immunomodulatory activity by altering the polarization state of polymorphonuclear neutrophils and ameliorating inflammatory responses in ischemia-reperfusion injury models. Additionally, 9-tert-Butyldoxycycline serves as a ligand for the "Tet-On" inducible gene expression system.

LasR-IN-2 blocks LasR via H-bond with TRY-56, useful in bacterial infection and CF research.

Anti-MRSA agent 23 (compound 11) is a potent agent against methicillin-resistant Staphylococcus aureus. This compound exhibits both antibacterial and antibiofilm properties. It facilitates the healing and reconstruction of MRSA-infected skin wounds by reducing bacterial load, alleviating inflammation, and promoting angiogenesis.

Antitubercular agent-23 combats Candida albicans (MIC: 1.1 μg/ml) and M. tuberculosis (MIC: 1 μg/ml).

Antibacterialagent 262 (compound A23) is a potent antibacterial agent that inhibits the activity of Xanthomonas oryzae pv oryzae. It also disrupts the integrity of bacterial cell membranes by preventing the formation of biofilms of Xanthomonas oryzae pv oryzae.

Ibafloxacine (R835) is a fluoroquinolone antibiotic that is used exclusively in veterinary applications and shows zero good bacteriostatic effect against

Enzyme-IN-3 disodium (compound 7) is a selective inhibitor of Mycobacterium tuberculosis shikimate kinase with an IC50 of 1.6 μM. Additionally, Enzyme-IN-3 disodium exhibits antibacterial properties.

DHFS-IN-1 (Compound 3) is an inhibitor of dihydrofolate synthetase (DHFS) with an IC50 of 2.6 μM. It is applicable for research into infectious diseases related to bacterial folate synthesis.

Alpibectir has antibacterial activity [1].

D-CS319 is a potent inhibitor of metal-𝛽-lactamases (MBLs), exhibiting IC50 values of 2.0 μM for IMP-1 and 3.0 μM for IMP-78. RPX 7546 possesses antibacterial activity.

Ph-Ph+ is a dimerized phenanthroline derivative with antitumor, antibacterial, and antifungal effects.

MtTMPK-IN-1 inhibits MtTMPK with 2.5 μM IC50, shows moderate anti-tuberculosis activity, and is low in cytotoxicity.

Quorum sensing-IN-9 (Compound 7d) inhibits quorum sensing in Pseudomonas aeruginosa by binding to the PqsR protein. It suppresses the expression of quorum sensing system-related genes lasB, rhlA, and pqsA, thereby preventing the production of virulence factors elastase, pyocyanin, and rhamnolipid. Quorum sensing-IN-9 disrupts the motility of P. aeruginosa, inhibits biofilm formation, and reduces the bacterium's virulence and pathogenicity. Additionally, it exhibits anti-infective activity in the Galleria mellonella larval model.

Compound 112: Powerful antibacterial, MIC 1250 μM against B. subtilis, E. coli, E. faecalis, S. typhimurium, S. aureus; also an HIV-1 antibody.

PptT-IN-2 inhibits PptT enzyme crucial in tuberculosis, with 2.5 μM IC50, showing potential in TB research.

MsbA-IN-4 (Compound 32) is a highly selective and potent inhibitor of MsbA (IC50: 3 nM).MsbA-IN-4 inhibits Escherichia coli (MIC: 12 μM).

Cefamandole (lithium), a second-generation broad-spectrum cephalosporin antibiotic, exhibits antimicrobial activity. Upon metabolism in the body, it releases free NMTT, which can lead to hypoprothrombinemia.

2-Bromo-2'-methoxyacetophenone acts as an irreversible inhibitor of MurA, effectively inhibiting MurA in E. coli with an IC50 of 0.38 μM. This compound helps inhibit bacterial cell wall synthesis, making it useful in antimicrobial research.

BioA-IN-1 (Compound 15) is an inhibitor of the key enzyme BioA in the biotin biosynthesis pathway of Mycobacterium tuberculosis, with an IC50 value of 0.195 μM. It exhibits antibacterial activity without cytotoxicity.

AVE-1330A sodium is a beta-Lactamase inhibitor.

Compound 174 (Compound 5g), an antibacterial agent, exhibits potent anti-infective properties in vivo along with appreciable pharmacokinetic profiles. This highly active substance demonstrates favorable biofilm removal capabilities, low hemolysis, and acceptable mammalian cell toxicity [1].

Gepotidacin (GSK-2140944) is a potent DNA topoisomerase inhibitor, a novel antibacterial efficacious against various anaerobes.

Levofloxacin mesylate is an orally active antibiotic effective against both Gram-positive and Gram-negative bacteria. It inhibits DNA gyrase and topoisomerase IV enzymes. Levofloxacin mesylate is employed in research related to chronic periodontitis, airway inflammation, and BK viremia. Additionally, it possesses anti-Orthopoxvirus activity.

Cephalosporin C exhibits relatively weak resistance to Gram-positive and Gram-negative bacteria. It is stable against penicillinase, but can be decomposed by cephalosporinase. When hydrolyzed to remove its side chain, it yields 7-amino-cefenoic acid (7-ACA), which is an essential raw material for the production of semisynthetic cephalosporins.

Fabimycin, a FabI inhibitor, combats drug-resistant gram-negative bacterial infections effectively.

Kalafungin inhibits various fungi, yeasts, protozoa, and gram-positive bacteria, less so for gram-negative bacteria.

LpxA-IN-1, a novel UDP-N-acetylglucosamine acyltransferase (LpxA) inhibitor exhibiting potent activity (IC 50 2 nM), effectively targets Pseudomonas aeruginosa

Antitubercular agent-15 (5n): low toxicity, fights M. tuberculosis strains; MIC90 values range 0.73-18.8 μg/mL.

Antimicrobial Agent-29 (Compound C35) influences the interaction between human hemoglobin and the Staphylococcus aureus IsdB hemophore. This compound facilitates the identification of IsdB:Hb PPI inhibitors [1].

Metallo-β-lactamase-IN-14 (Compound 17e) serves as an inhibitor of Metallo-β-Lactamase, displaying inhibitory activity against VIM-1 and VIM-2. This compound also exhibits antibacterial effects on Gram-negative (GN) bacteria and P. aeruginosa [1].

MsbA-IN-5 (compound 40) is a potent and highly selective inhibitor of MsbA (IC50: 2 nM). MsbA-IN-5 can be used in Gram-negative studies.

Antibiofilm agent-14 (compound 11) functions as an antibiofilm agent. It exhibits antifungal activity against C.albicans SC5314, with a minimum inhibitory concentration (MIC) of 50 μM.