Antibactérien

Piperacillin hydrate is a semisynthetic broad-spectrum β-lactam antibiotic. It exhibits potent bactericidal activity against Gram-negative bacteria and some Gram-positive bacteria by targeting penicillin-binding proteins. Piperacillin hydrate is frequently combined with the β-lactamase inhibitor Tazobactam for enhanced efficacy.

Antibacterial agent 169 (Compound 28), a pyrrolamide-type GyrB/ParE inhibitor, exhibits antibacterial properties by inhibiting Gyrase and Topo IV in Staphylococcus aureus. It has IC 50 values of 49 nmol/L and 1.513 μmol/L, respectively [1].

MsbA-IN-2 is a potent inhibitor of the lipopolysaccharide transporter MsbA and is able to act on E. coli MsbA (IC50: 2 nM).

Nitrovin is an antimicrobial growth promoter that induces ROS-mediated non-apoptotic and quasi-apoptotic cell death by targeting TrxR1. It exhibits anticancer activity with IC50 values ranging from 1.31 to 6.60 μM for both tumor and normal cells.

PptT-IN-1, a potent PptT inhibitor (IC50: 2.8 μM), shows promise for tuberculosis research.

Carumonam Sodium is a monobactam, penicillin-binding protein inhibitor. It is used as antibacterials.

EFP-IN-1: potent β-lysine derivative, inhibits EFP, slows E. coli growth.

Keto lovastatin is an impurity of lovastatin with antibacterial properties. Lovastatin is a cell-permeable HMG-CoA reductase (HMG-CoA reductase) inhibitor used to reduce cholesterol levels.

Urease-IN-20 (compound XBP2) is an inhibitor of Helicobacter pylori (H. pylori), with an IC50 of 0.14 μM for H. pylori inhibition. It effectively decreases apoptosis in GES-1 cells infected with H. pylori and reduces levels of ROS and γH2AX. Urease-IN-20 also demonstrates significant gastric mucosal protective effects, making it suitable for H. pylori research.

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

Anti-MRSA agent 2 inhibits MRSA at 0.098 μg/ml, with low toxicity and disrupts bacterial membranes and DNA.

NDM-1 inhibitor-3 is a New Delhi Metallo-β-lactamase-1 (NDM-1) inhibitor (Ki : 4 μM) widely found in nature and is associated with antibiotic resistance.

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

Eravacycline (TP-434) is a potent and broad-spectrum antibacterial agent.

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

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

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.

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.

(4-Aminobenzoyl)-D-glutamic acid (Compound 17) exhibits competitive inhibitory activity against the H2-pterin synthesis system, affecting folic acid synthesis and subsequently inhibiting bacterial growth.

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.

Antifungal agent 27 shows moderate action against MRSA, weak against C. albicans, with MICs of 8 μg/mL and 32 μg/mL, respectively.

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

Antibacterial agent 80 (compound 20) has antibacterial activity [1].

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

MRL-436 is an RNA polymerase inhibitor with antibacterial activity. Its effectiveness depends on the β' subunit and the 622nd residue of the RNAP ω subunit. MRL-436 can inhibit Rifampicin-resistant RNA polymerase derivatives and shows antibacterial activity against Rifampicin-resistant strains.

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

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].

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

Bilanafos is an agent of Anti-Bacterial.

InhA-IN-7 (Compound 11), a derivative of Triclocan, shows inhibitory activity against enoyl-acyl carrier protein reductase (InhA) with an IC50 of 96 nM. It effectively inhibits the proliferation of both wildtype and mutant strains of Mycobacterium tuberculosis, exhibiting minimum inhibitory concentrations (MICs) ranging from 19 to 75 μM [1].

AAA-10 formic is an orally active inhibitor of intestinal bacterial bile salt hydrolase (BSH) against B.

Metallo-β-lactamase-IN-16 (compound 18), a sulfone-containing metallo-β-lactamase inhibitor, exhibits antimicrobial activity. It effectively inhibits various metallo-β-lactamases, including NDM-1 (New Delhi metallo-β-lactamase-1), IMP-1 (imipenemase-1), VIM-1 (Verona Integron-encoded Metallo-β-lactamase), and VIM-2. The IC50 values for these enzymes are 0.16 nM, 0.23 nM, 0.31 nM, and 1.0 nM respectively.

Mycobacterium Tuberculosis-IN-6 (compound b1) is an inhibitor of the enoyl reductase InhA from Mycobacterium tuberculosis, with an IC50 value of 7.74 μM. It is useful in antibacterial research.

(E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium TFA (Compound 4a) functions as a Gram-negative outer membrane permeabilizer by targeting Met47 in LptA to disrupt LptA/LptC interactions, exhibiting synergistic antibacterial activity. This compound, when in the form of (trifluoromethanesulfonate), enhances the efficacy of pol B against both wild-type and multi-drug resistant A. baumannii and E. coli strains. Additionally, (E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) serves as an adjuvant for antibiotics combating multi-drug resistant Gram-negative bacteria.

Antibacterial Agent 172 (Compound 6a), a Clostridioides difficile (Cd) SpoVD inhibitor with an IC50 value of 89 nM, effectively inhibits the sporulation of Clostridioides difficile. It is useful for research on bacterial infections [1].