Antibactérien

7-Hydroxytropolone (3-Hydroxytropolone) is an antibiotic that exhibits activity against Gram-positive and Gram-negative bacteria, as well as yeasts and fungi. It also functions as an inhibitor of 2''-O-adenylate transferase.

Avibactam sodium dihydrate (NXL-104) is a reversible covalent inhibitor for CTX-M-15 and TEM-1 β-lactamases with IC50s of 5 nM and 8 nM.

RNAP-σ interaction inhibitor-2 (compound 7d) is an inhibitor targeting the interaction between RNA polymerase and the sigma factor. It demonstrates inhibitory activity against S. aureus with a minimum inhibitory concentration (MIC) of 2 µg/mL.

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

PF 03709270 is an oral prodrug of sulopenem with broad-spectrum antibacterial effects on gram-positive and gram-negative bacteria.

MB076 is an innovative heterocyclic triazole designed with enhanced plasma stability. It effectively inhibits seven distinct Class C Acinetobacter-derived cephalosporinases (ADCs) β-lactamase variants with K i values less than 1 μM. Additionally, MB076 demonstrates a synergistic effect when combined with various cephalosporins to restore pBCSK(−) susceptibility [1].

MraY-IN-2 (compound 6) is an effective inhibitor of bacterial transposase MraY (IC50=4.5 μ M), and can be used for antibacterial research.

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

Cefoxazole is a β-lactam antibiotic featuring an isoxazole structure, known for its antibacterial activity. It can be utilized in the study of infectious diseases.

Anti-MRSA agent 6 (compound 3q6) is a potent anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) agent with low cytoxicity for MCF-7, A549 cells [1].

Compound 8b inhibits VEGFR-2/DHFR, combats various bacteria, and fights cancer cells.

(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.

Antibacterialagent 279 (compound A12) is an effective antibacterial agent. It inhibits the SOS response of Pseudomonas aeruginosa.

BM635 mesylate inhibits MmpL3; kills Divergent bacterium with 0.6 µM MIC50; boosts bioavailability.

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].

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

G092 is a potent inhibitor of MsbA. MsbA is an ABC transporter protein. G092 has potential for antibacterial drug research.

MtMetAP1-IN-1 is an inhibitor of methionine aminopeptidase 1 ( MetAP1 ). MtMetAP1-IN-1 shows antimycobacterial activity.

<p>MtTMPK-IN-3 inhibits Mycobacterium tuberculosis kinase with IC50 0.12μM, MIC 12.5μM on Mtb, cytotoxic EC50 12.5μM on MRC-5 cells.</p>

Kendomycin is a proteasome inhibitor and endothelin receptor antagonist. It induces apoptosis in lymphoma.