Antibacteriano

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

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

K13787 is an acetohydroxy acid synthase (AHAS) inhibitor with antibacterial properties. It exhibits antimicrobial activity against various non-tuberculous mycobacteria (NTM) as well as clarithromycin (CLR) resistant strains.

FtsZ-IN-13 (Compound C11) functions as an inhibitor of the temperature-sensitive mutant Z (FtsZ), exhibiting IC50 values of 47.97 μM for FtsZSa and 34 μM for FtsZPa. It demonstrates notable antibacterial activity against Staphylococcus aureus (with a minimum inhibitory concentration of 2 μg/mL), cystic fibrosis Staphylococcus aureus clinical isolates, and methicillin-resistant Staphylococcus aureus (MRSA). FtsZ-IN-13 is applicable in research on antibiotic resistance.

Antibacterialagent 259 (K3) is a bactericide with EC50 values of 1.5, 1.7, and 4.9 mg/L against Xoo, Xoc, and Xac, respectively. It induces the production of reactive oxygen species (ROS) in pathogens, leading to their death. Antibacterialagent 259 is applicable in research for controlling bacterial diseases in plants.

Fenbenicillin (Phenbenicillin) potassium is a semi-synthetic penicillin with antibacterial spectrum activity.

Compound 3d: antitubercular, MIC 0.007 μg/mL vs MTB H37Rv, 1.851 μg/mL vs MDR-MTB 16833, metabolically unstable.

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.

Rubropunctatin is a monascus pigment with very potent cancer cell proliferation inhibitory effects.

Ro 24-4383 is a carbamate-linked dual-action antibacterial agent.

RmlA-IN-2: Strong RmlA blocker, hinders l-rhamnose synthesis & alters bacterial wall permeability (IC50: 0.303 μM).

Antibacterial agent 118, potent against various mycobacteria, has MIC values ranging from 10.2 to 163.0 μM. Useful in TB research.

LpxC-IN-10 is a selective LpxC inhibitor with an MIC of 0.5 μg/mL against E. coli and K. pneumoniae and is capable of being used to study bacterial infections.

<p>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.</p>

MtTMPK-IN-8 inhibits MtbTMPK, has low cytotoxicity, shows 0.78-9.4 μM activity against Mycobacterium, useful for tuberculosis research.

(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.

HldA/E-IN-1 (compound 8) is a dual inhibitor of HldA/E, exhibiting IC50 values of 17.2 μM and 67.8 μM, respectively. This compound is utilized in research on antibacterial infections.

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

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.

MBX-1162, a bis-indole compound, has demonstrated unique substrate specificity related to MepA and MepR in studies investigating its resistance mechanisms in Staphylococcus aureus. It has not shown cross-resistance with related compounds.

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.

ACHN-975: potent LpxC inhibitor with subnanomolar activity; targets many gram-negative bacteria; MIC ≤1 μg/mL.

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

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

MtDTBS-IN-1 is a notably potent binder (K_D = 57 nM) and inhibitor (K_i = 5 μM) of MtDTBS.

(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.

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.

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.

PqsR-IN-2, potent PqsR inhibitor, curbs Pseudomonas aeruginosa communication, reduces pyocyanin, with low toxicity.

FR-145715 is a histamine H2 receptor antagonist characterized by its specific anti-Helicobacter pylori activity. This compound is utilized in the study of gastric lesions.

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

Anti-MRSA agent 3 targets MRSA with 0.098 μg/ml MIC, low toxicity, binds DNA, and disrupts cell walls/membranes.

<p>Doxazosin impurity 12 acts as an inhibitor of CTX-M β-lactamase (Beta-lactamase) with a Ki value of 0.7 mM against CTX-M.</p>

2'-Amino-2'-deoxyadenosine (9-(2-Amino-2-deoxypentofuranosyl)-9H-purin-6-amine) is a nucleoside antibiotic that effectively inhibits various Mycoplasma strains.

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

BWC0977 is an effective topoisomerase inhibitor that disrupts bacterial DNA replication by targeting both DNA gyrase and topoisomerase IV. The minimum inhibitory concentration (MIC90) of BWC0977 against MDR (multi-drug resistant) Gram-negative bacteria ranges from 0.03 to 2 µg/mL.

MraY-IN-3 (12a) is a potent inhibitor of the bacterial translocase MraY (IC50: 140 μM). 46 μg/ml).

QPX7728 bis-acetoxy methyl ester is an inhibitor of boronic acid β-lactamase.

TBAJ-5307 is a broad-spectrum anti-non-tuberculous mycobacteria inhibitor that targets the FO-domain of the engine, preventing rotation and proton-translocation. TBAJ-5307 inhibits non-tuberculous mycobacteria in vitro and in vivo [1].

BDM91288, an orally active AcrB efflux pump inhibitor of pyridinium piperazine, enhances the in vivo efficacy of levofloxacin in treating Klebsiella pneumoniae pulmonary infection in mouse models [1].

Cetefloxacin (E 4868) is a broad-spectrum antibacterial antibiotic with a minimum inhibitory concentration (MIC) ranging from 0.007 to 8 µg/ml. In mice, cetefloxacin demonstrates favorable pharmacokinetic properties and provides protection against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus pneumoniae.

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.

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

SPR719 is an inhibitor of gyrase B, has bactericidal activity.

NDM-1 Inhibitor-5 (compound 57) exhibits strong inhibition of NDM-1, characterized by a K i of 2.5 μM. Additionally, it demonstrates synergistic antibacterial effects when combined with meropenem [1].

Bilanafos is an agent of Anti-Bacterial.

Aeroplysinin I is an antibacterial compound from the sponge. It has cytotoxic activity against colon cancer cells by promoting β-catenin degradation.

<p>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].</p>

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