Antibacteriano

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

LasR-IN-3 inhibits LasR in Pseudomonas, disrupting its dimer, causing loss of function.

Lapyrium chloride (Emcol E 607) is a broad-spectrum antibacterial agent that serves as a preservative and disinfectant.

Aztreonam-siderophore conjugate 63 is an antibacterial agent that exhibits efficacy against Gram-negative bacteria through the linkage of aztreonam to a

DNA gyrase B-IN-1, a potent inhibitor of P. aeruginosa DNA gyrase B, has IC50 of 2.2 μM with high affinity and stability.

(1S,2R,7S)-Sitafloxacin (DU-6856) is an enantiomer of Sitafloxacin and functions as a topoisomerase inhibitor. As an antibiotic, it demonstrates inhibitory activity against Escherichia coli DNA gyrase (IC50 0.18 μg/mL) and Staphylococcus aureus topoisomerase IV. (1S,2R,7S)-Sitafloxacin exhibits antibacterial properties and is utilized in the study of various bacterial infections.

(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.

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

<p>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].</p>

NusB-IN-1 (22r) is an oral bacterial rRNA inhibitor, effective against MRSA and VRSA.

Lambertellin, an effective antibiotic, acts as both a bactericide and fungicide. It exerts anti-inflammatory effects in LPS-stimulated RAW 264.7 macrophages by modulating the activation of MAPK and NF-κB signaling pathways.

O-1269 acts as a partial agonist for the cannabinoid receptor 1 (CB1R), with a binding affinity (Ki) of 32 nM. Additionally, it exhibits analgesic properties.

Antibacterial agent 90 (6n), a pleuromutilin derivative, targets Gram-positive pathogens and Mycoplasma pneumoniae.

Pneumolysin-IN-1 (compound PB-3), characterized as a targeted small molecule inhibitor of Pneumolysin (PLY) with an IC50 value of 3.1 µM, acts as a pore-blocking agent and an anti-virulence factor. This compound is useful for researching infections caused by Streptococcus pneumoniae [1].

Palmitanilide (Palmitic acid anilide) is an antimicrobial agent effective against Gram-positive bacteria. It can electrostatically bind to components of the cell wall of Gram-positive bacteria (such as Bacillus cereus), altering the membrane structure and affecting normal cellular functions. Palmitanilide shows potential for research into infections caused by Gram-positive bacteria.

MK-3402 is a metallo-beta-lactamase inhibitor. MK-3402can be used in the research of bacteria .

<p>Mazethramycin is an antitumor antibiotic that exerts its effects by disrupting DNA replication and RNA synthesis within cells. It is utilized in cancer research.</p>

Squalamine lactate is an aminosterol compound discovered in the tissues of the dogfish shark, with antimicrobial activity.

MA220607 is an antibacterial agent characterized by low hemolytic toxicity and a dual-target mechanism of action (MOA). It promotes FtsZ protein polymerization, increases bacterial membrane permeability, and inhibits biofilm formation. The resistance rate of MA220607 is low, with MICs against Gram-positive bacteria and Gram-negative bacteria ranging from 0.062-2 μg/mL and 0.5-4 μg/mL, respectively [1].

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