Antibacteriano

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

Elongation factor P-IN-2, a β-lysine derivative, is a potent EFP inhibitor reducing E. coli growth.

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

VEGFR-2/DHFR-IN-2 inhibits VEGFR-2 & DHFR (IC50: 0.623 & 9.085 μM), toxic to C26, HepG2, MCF7 cells (IC50: 3.59-8.38 μM), promising for cancer study.

(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.

BM635 hydrochloride, an MmpL3 inhibitor, strongly blocks Divergent bacteriophage H37Rv (MIC50: 0.08 μM), with doubled in vivo potency.

Apalcillin (PC-904) combined with Ro 48-1220 (a penicillin sulfone β-lactamase inhibitor) exhibits broad-spectrum activity against Gram-negative aerobic and anaerobic bacteria, excluding Klebsiella acid-producing strains. This combination shows strong efficacy against β-lactamase-producing Moraxella catarrhalis, Haemophilus influenzae, and Neisseria gonorrhoeae with an effective MIC of 11 μg/mL. Additionally, it inhibits Pseudomonas aeruginosa, Stenotrophomonas maltophilia, and Acinetobacter at low MICs (0.25 to 4 μg/mL). However, it has limited efficacy against oxacillin-resistant staphylococci and some Gram-positive bacteria. Apalcillin/Ro 48-1220's effectiveness against certain extended-spectrum β-lactamase-producing Escherichia coli is comparable to piperacillin/tazobactam, though it is less effective against SHV-type β-lactamases.

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

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

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

Antibiofilm agent-4 is a LasR inhibitor, demonstrating optimal antibiofilm and anti-QS (quorum sensing) properties.

7-APRA is a semisynthetic intermediate of the cephalosporin class of antibiotics. It exhibits antibacterial activity and is primarily used in the synthesis of other cephalosporin antibiotics, such as Cefaclor and Cefprozil.

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

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.

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.

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

QPX7728 is an of ultra-broad-spectrum boronic acid beta-lactamase.

(E)-Cefodizime ((E)-THR-221) is an antibiotic that selectively binds to penicillin-binding proteins (PBPs), inhibiting bacterial cell wall synthesis, which results in its antibacterial activity. It holds potential for research into various bacterial infections, including the prevention of preoperative infections.