Antibatterico

DuP-721: broad-spectrum, oral antibiotic targeting various bacteria, including M. tuberculosis.

4-Nitrophenyl palmitate serves as a colorimetric substrate for lipase and esterase, enabling the quantification of enzyme activity through the release and colorimetric detection of 4-nitrophenol at 410 nm following enzymatic hydrolysis. This compound facilitates the characterization of enzyme activity across diverse bacterial and mammalian sources, including Burkholderia and porcine pancreatic lipases.

β-Lactamase-IN-2 is an inhibitor of β-Lactamase with anti-microbial and anti-bacterial effects.

MsbA-IN-6: potent antibiotic, hinders MsbA in gram-negative bacteria, kills E. coli, effective on drug-resistant strains.

Sudoterb free base (Sudoterb) , also known as LL3858, is an anti-tubercular drug candidate.

IpOHA is a potent inhibitor of plant KARI and functions as an antimycobacterial agent, demonstrating a K_i value of 97.7 nM against Mycobacterium tuberculosis (

A 33853 is an antibiotic isolated from culture broth of Streptomyces sp.

L-Methioninamide hydrochloride is a potent inhibitor of methionyl-tRNA synthetase that reduces the toxicity of CDDP.

DNA Gyrase-IN-8 is a potent inhibitor of DNA gyrase, demonstrating antimicrobial activity with an IC50 of 8.45 µM [1].

Netropsin dihydrochloride, a small MGB, blocks topoisomerase I/II, hindering cleavable complex stabilization.

17(R)-Resolvin D4 (17(R)-RvD4) is an epimer of RvD4, generated through the aspirin-induced modification process.

Urease Inhibitor 07 is an isosubstituted metalloproteinase inhibitor with potential activity against Mycobacterium tuberculosis strain H37Rv.

DNA gyrase B-IN-3 (Compound A), with an IC50 of less than 10 nM, acts as an inhibitor of bacterial DNA gyrase B and exhibits antibacterial activity against Gram

DHFR-IN-10 (compound 4c) is a potent inhibitor of dihydrofolate reductase (DHFR), displaying an inhibition concentration half-maximum (IC50) of 4.21 μM against

AB131, an inhibitor of MSMEG 6649 and Rv2172c (KD values of 0.16 and 0.02 μM, respectively), enhances the antimycobacterial efficacy of the antitubercular agent

Flurofamide is an effective bacterial urease inhibitor and has potential in the treatment of infected urinary calculi.

Tylvalosin (Acetylisovaleryltylosin) is a broad-spectrum macrolide antibiotic with antibacterial and antiviral properties, effective against PRRSV infection.

Antibacterial 91: Inhibits aaRS, IC50 2.10μM vs. S. enterica ThrRS, has antibacterial properties. [1]

Antibiofilm Agent-2 (Compound 4T) serves as a potent biofilm inhibitor, exhibiting an IC50 of 3.6 μM, and impairs the quorum sensing system along with iron

Isotianil is a plant defense inducer that activates typical plant defense responses without direct antimicrobial effects, serving as a plant protection agent

Antituberculosis Agent-1 (Compound 8a) is an effective antituberculosis agent, demonstrating a minimum inhibitory concentration (MIC) of 3.84 μg/mL against

WQ 2743 is a potent agent of antimicrobial.

Photosensitizer-1 shows promise in treating infections, effective against S. aureus in mouse wounds.

Cefteram (T-2525), an orally active ester of the cephalosporin class, is the free acid form of Cefteram pivoxil.

NSC309401 is an E. coli dihydrofolate reductase inhibitor with an IC50 value of 189 nM and a dissociation constant (Kd) of 14.57 nM [1].

BDM91270 (compound 29) serves as an inhibitor of the E.

G43-C3-TEG is a glycosyl-transferase inhibitor that diminishes biofilm formation by inhibiting the synthesis of extracellular polysaccharides (EPS) [1].

Tuberculosis inhibitor 7 (compound 2d), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, exhibits potent activity against Mycobacterium tuberculosis and

Compound 158 (6c), a Micrococcin analogue, serves as an antibacterial agent effective against impetigo and Clostridium difficile infection (CDI) [1].

Sphinganine (d16:0 branched), an aniso-branched sphingolipid, is identified as a constituent of ceramide-containing phospholipids in bacteria.

1,8-Dichloroanthraquinone, a derivative of anthraquinone, effectively inhibits sulfide production in sulfate-reducing bacteria [1].

Rosoxacin (Acrosoxacin) shows antibacterial activities against a broad spectrum of Gram-negative bacteria including Neisseria gonorrhoeae (MIC90 = 0.03mg/ml).

Valnemulin, a broad-spectrum pleuromutilin antibiotic, targets peptidyl transferase within the 50S ribosomal subunit, effectively used in veterinary medicine to address swine diseases such as B. hyodysenteriae and M. hyopneumoniae.

Variculanol, a compound with antimicrobial, anticancer, and anti-HCV NS3/4A protease properties, is derived from the marine fungus Aspergillus versicolor [1].

Aminoacyl tRNA synthetase-IN-1 is an inhibitor of bacterial aminoacyl tRNA synthetase (aaRS).

Antituberculosis agent-6: potent against M. tuberculosis (MIC 3.49 μM), antifungal (MIC 62.5 μM), high GI absorption.

Despropylene gatifloxacin, a metabolite of AM-1155, exhibits potent antibacterial activity and has favorable pharmacokinetics [1].

Δ2-transEicosenoic acid, an α,β-unsaturated fatty acid, emerges as a by-product during the synthesis of Δ2-ciseicosenoic acid, which along with its salts, shows promise in diabetes treatment and lipid metabolism enhancement. Additionally, the compound 2-octadecenoic acid is recognized for its ability to enhance liver function and reduce blood sugar levels in streptozocin-induced diabetic rats.

Tuberculosis inhibitor 6 (compound 2c), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, is highly active against Mycobacterium tuberculosis (MIC 90 of

SA09-Cu is a potent, noncompetitive inhibitor of NDM-1, with an IC50 of 9.6 nM.

DQn-1, a potent antifolate, demonstrates efficacy against Mycobacterium tuberculosis (Mtb) with an MIC 90 of 0.03 µM.

Zabofloxacin inhibits bacterial topoisomerases II/IV, effectively targeting gram-positive pathogens like S. aureus and S. pneumoniae.

Urease-IN-6, a potent Urease inhibitor, exhibits an IC50 value of 14.2 μM and is utilized in the research of peptic and gastric ulcers [1].

Lithium benzoate, an aromatic alcohol present in numerous plants, commonly serves as an additive in food, beverages, cosmetics, and various other products. This compound exhibits antibacterial and antifungal properties, functioning effectively as a preservative [1].

Bio-AMS is a potent inhibitor of bacterial biotin protein ligase, exhibiting selective activity against Mycobacterium tuberculosis (Mtb) and disrupting fatty

Avarol triggers cell death in pancreatic cancer and is a non-toxic, neuroprotective AChE inhibitor for Alzheimer's.

β-L-Gulopyranosyl-caldarchaetidyl-glycerol is the principal polar lipid in the archaeon T. acidophilum. Its cellular levels in T. acidophilum HO-62 show a positive correlation with culture pH and a negative correlation with temperature. This compound also serves as a standard for polar lipid quantification from T. acidophilum HO-62. [Matreya, LLC. Catalog No. 1303]

Trovafloxacin: broad-spectrum fluoroquinolone, blocks DNA gyrase/topoisomerase IV and PANX1 channel (IC50=4μM).

Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide derived from bovine lactoferrin spanning residues 17-41, exhibits broad-spectrum antimicrobial properties against Gram-positive and Gram-negative bacteria, viruses, protozoa, and fungi. Additionally, this compound demonstrates antitumor activities [1] [2].

T145 halts key bacteria growth at sub μg/ml, deters resistance, and may enhance drug lifespan.

CPFX2090, a cephalosporin antibacterial compound.

L 680833 is an orally active monocyclic beta-lactam human polymorphonuclear leukocyte elastase inhibitor.

Sulfisoxazole acetyl (Gantrisin) is an agent with antibacterial activity.

TH-Z145 is a potent FPPS inhibitor for the study of myeloma and lung cancer.

4-Aminobenzylphosphonic acid, an inhibitor of alkaline phosphatase (Ki= 1.1 mM for the bovine intestine enzyme), is utilized in affinity chromatography for alkaline phosphatase purification and in the electrochemical modification of glassy carbon electrodes.

AG 85 is a major secretion protein of Mycobacterium tuberculosis.

NSC309401 is an E. coli dihydrofolate reductase inhibitor, displaying potency with an IC50 value of 189 nM and a dissociation constant (KD) of 14.57 nM [1].

DprE1-IN-9 (compound B18) is an efficient reversible inhibitor of DprE1, interacting with the enzyme's receptor cavity.

Pristinamycin IA (Mikamycin B) is a substrate for the P-glycoprotein and a cyclo-peptidic macrolactone antibiotic.

Contezolid (MRX-I) is an antibiotic with bactericidal activity and can be used to study tuberculosis.

A7132 is an antibacterial agent and possesses broad and potent antibacterial activity.

Salicyl-AMS is an inhibitor of mycobacterium auxin biosynthesis that inhibits the growth of mycobacterium in the presence of iron deficiency in vitro.

Supercinnamaldehyde is a potent activator of transient receptor potential ankyrin 1 (TRPA1), exhibiting an EC50 of 0.8 μM, and induces activation of TRPA1 ion

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

(R)-ZG197: Activates Sa ClpP (EC50=1.5μM) & Hs ClpP (EC50=31.4μM); selective for Sa ClpP.

PptT-IN-2 inhibits PptT enzyme crucial in tuberculosis, with 2.5 μM IC50, showing potential in TB research.

Urease-IN-2 is a non-competitive inhibitor of urease (IC50: 0.94 μM, Ki: 1.6 μM) that non-competitively inhibits Jack bean urease (JBU).

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

LY 215890 is a compound that exhibits potent Gram-negative and Gram-positive antibacterial activity.

Gougerotin is an inhibitor of protein synthesis.

MCB-3681, active against gram-positive bacterium, is the antibacterial Oxaquin's active substance.

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.

Anticaries agent-1 (Compound 21b) is utilized as an anticaries agent. It effectively inhibits biofilm formation with an IC50 of 77 μM and restricts the growth of S. mutans.

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.

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.

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

β-Glucuronidase-IN-3 (Compound 49) is a covalent allosteric inhibitor targeting β-glucuronidase. It exhibits potent inhibitory activity against Escherichia coli β-glucuronidase (EcGUS) with an IC50 of 12.9 nM. The compound exerts its inhibitory effect through reversible covalent modification of cysteine residues (Cys28, Cys443, and Cys197) on EcGUS. It is applicable in research on gut microbiota-related diseases, particularly in reducing the toxic side effects of Irinotecan and non-steroidal anti-inflammatory drugs (NSAIDs).

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.

DC-159a, an 8-methoxy fluoroquinolone, possesses broad-spectrum antibacterial activity, with a particular efficacy against Gram-positive pathogens. The MIC90 values for DC-159a are 0.5 μg/mL against Streptococcus anginosus group, 4 μg/mL against Clostridium difficile, and 2 μg/mL against Bacteroides fragilis.

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

Antimicrobial agent-38 (compound 10) effectively inhibits methicillin-resistant Staphylococcus aureus (S. aureus) strain ATCC 700699 and non-resistant strain ATCC 29213, with minimum inhibitory concentrations (MIC) of 32 mg/L and 64 mg/L, respectively.

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

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

Colistin adjuvant-1, inhibits NF-κB (IC50: 0.209 μM), boosts mucin against gram-negative bacteria.

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

Compound 11: Sulfonylurea derivative, antimicrobial, anticancer; MIC 0.039-0.156 mg/mL; A549 IC50: 19.7 μg/mL, PC3 IC50: 11.9 μg/mL.

KKL-40 is a small-molecule inhibitor that targets the trans-translation process, effectively suppressing methicillin-sensitive and resistant Staphylococcus aureus (S. aureus) and other Gram-positive pathogens, including vancomycin-resistant Enterococcus faecium, Bacillus subtilis, and Streptococcus pyogenes. It works in synergy with the human antimicrobial peptide LL-37 to inhibit S. aureus, but does not show synergistic effects with other antibiotics such as daptomycin, kanamycin, or erythromycin. KKL-40 inhibits trans-translation, an extreme form of recoding, while being non-toxic to HeLa cells.

DNA ligase-IN-2 (compound 2) acts as a potent LigA inhibitor, effectively hindering the DNA-independent spontaneous adenylation activity of full-length LigA and the truncated enzyme LigA:AD with an IC50 of 29 nM. It also significantly suppresses the in vitro growth of Staphylococcus aureus, showing MIC values of 1 μg/mL for S. aureus ATCC 29213 and S. aureus ATCC 700699, while the MIC for Escherichia coli (E. coli) ATCC 25922 is >64 μg/mL.

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.

LpxH-IN-2 (compound 014), a potent inhibitor of LpxH, exhibits antibacterial activity against E. coli.

NS-062 is an orally effective, irreversible covalent inhibitor targeting EGFR, demonstrating antiproliferative activity in the resistant double mutant H1975 cells with an IC50 of 0.19 μM. It also exhibits antitumor activity in a murine H1975 xenograft model.

DRF-8417 is an oxazolidinone antibiotic, active against both Gram-positive bacteria and fastidious Gram-negative bacteria. The MIC50 and MIC90 values of DRF-8417 for Gram-positive pathogens range between 0.06-1 mg/L.

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.