Antibiotiques

<p>N-Acetylpurinomycin is a selective agonist of CB2 receptor.</p>

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

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

<p>N-(3-Oxobutanoyl)-L-homoserine lactone (3-oxo-C4-HSL) serves as an autoregulator for carbapenem antibiotic biosynthesis in Erwinia carotovora ATCC 39048 and induces the expression of rhiI in R. leguminosarum [1].</p>

Gusperimus trihydrochloride is a derivative of the antitumor antibiotic spergualin with immunosuppressant activity.

<p>OM173-αA is a quinone bacterial metabolite that inhibits the growth of the bacteria M.</p>

<p>Annamycin, a semi-synthetic doxorubicin derivative, binds DNA, blocks topoisomerase II, and evades MDR, inhibiting DNA/RNA/protein synthesis.</p>

S-Adenosylhomocysteine (SAH) hydrolase is responsible for the reversible hydrolysis of SAH into adenosine and homocysteine. Inhibition of this enzyme leads to the accumulation of SAH within cells, thereby increasing the SAH to S-adenosylmethionine (SAM) ratio and subsequently inhibiting SAM-dependent methyltransferases. (−)-Neplanocin A, a potent and irreversible inhibitor of SAH hydrolase (Ki= 8.39 nM), exhibits significant antitumor activity against mouse leukemia L1210 cells and holds broad-spectrum antiviral properties. Its efficacy notably surpasses that of the reversible inhibitor 3-deazaneplanocin, especially in combating vesicular stomatitis, evidencing a higher potency with ID50 values of 0.07 μg/ml for Neplanocin A versus 0.3 μg/ml for 3-deazaneplanocin.

Myxopyronin A is an inhibitor of bacterial RNA polymerase.

Alatrofloxacin is a prodrug of trovafloxacin.

<p>Caerulomycin A (Caerulomycin) (Cerulomycin; Caerulomycin) is an antifungal compound.</p>

<p>Desoxymycin is an antibiotic product that belongs to the class of aminoglycosides, which is derived from natural sources such as certain species of Streptomyces bacteria. This compound exhibits its mode of action by specifically binding to the bacterial ribosomal RNA, interfering with protein synthesis. As a result, it inhibits the replication and growth of susceptible bacterial strains.</p>

<p>Amoxicillin is an aminopenicillin antibiotic and is used for the treatment of various bacterial infections. It works by inhibiting the synthesis of bacterial cell wall mucopeptides, leading to cell lysis and death</p>

<p>N-Acetylamphotericin B is a derivative of the well-known antifungal agent Amphotericin B, which is derived from the bacterium *Streptomyces nodosus*. This compound is an acetylated version of Amphotericin B, designed to improve certain pharmacokinetic properties. It operates by binding to ergosterol, a key component of fungal cell membranes, leading to the formation of pores that disrupt membrane integrity, causing cell death. The acetylation is intended to reduce the compound's cytotoxicity and improve its solubility in aqueous solutions, potentially allowing for enhanced therapeutic applications.</p>

<p>Carumonam is a synthetic monobactam antibiotic, which is derived from chemically modifying aztreonam to enhance its antimicrobial properties. Its source is entirely synthetic, allowing for precise structural modifications to target specific bacterial pathogens. The mode of action involves the inhibition of bacterial cell wall synthesis. Carumonam binds to penicillin-binding proteins (PBPs) on the surface of bacterial cell walls, disrupting the peptidoglycan cross-linking process necessary for cell wall strength and integrity. This action results in bacterial cell lysis and death, making it effective against a range of Gram-negative bacteria.</p>

Toxoflavin (Xanthothricin) is an antagonist of transcription factor 4 (TCF4)/β-catenin complex. Toxoflavin also acts as an inhibitor of KDM4A.

<p>Gramicidin S hydrochloride is a cyclic peptide antibiotic, which is a derivative of the naturally occurring antibiotic gramicidin S. It is sourced from Bacillus brevis, a type of soil bacterium. This peptide operates through a unique mode of action, whereby it disrupts bacterial cell membranes. By integrating into the lipid bilayer, it increases membrane permeability, leading to leakage of essential ions and molecules, and ultimately causing cell death.</p>

<p>Oleandomycin is a macrolide antibiotic, which is derived from the bacterium *Streptomyces antibioticus*. This antibiotic functions by binding to the 50S subunit of the bacterial ribosome, thereby inhibiting protein synthesis. The interruption of this essential process ultimately leads to the cessation of bacterial growth and replication.</p>

<p>Acetomycin, a γ-lactone from S. ramulosus, halts HCT-8 colon and L1210 leukemia cell growth.</p>

CRS-3123, a methionyl-tRNA synthetase inhibitor, is used potentially for the treatment of enteric infections.

Potent, selective CHS inhibitor with 0.12 mM IC50; effective against drug-resistant fungi.

<p>Amicoumacin A has antibacterial activity. It also strongly suppresses inflammatory and ulcer activity.</p>

<p>Neocryptolepine-Cl (compound Z24) is an inhibitor of Bcthi4, demonstrating excellent antifungal activity against B. cinerea, with an EC50 value of 0.56 μg/mL.</p>

Pibrozelesin, a water-soluble duocarmycin B2 derivative, binds AT-rich DNA, blocking replication and inducing cell death.

Imidocarb dihydrochloride monohydrate is an effective antiprotozoal agent against the parasite B. bovis (IC50: 87 μg/ml).

<p>Mal-PEG4-VA-PBD is a drug-linker conjugate for Antibody-Drug Conjugates (ADCs), comprising the antitumor antibiotic Pyrrolobenzodiazepine (PBD), connected</p>

<p>Saroaspidin B is a dimeric form of a biphenyl triphenol, characterized as an antibiotic compound.</p>

<p>Saptomycin E is an antitumor antibiotic.</p>

<p>2-Acetyl-2-decarboxamidotetracycline is a tetracycline-class antibiotic. It exhibits a UV absorption spectrum similar to that of tetracycline or 5-oxytetracycline at concentrations above 300 mμ, characteristic of the BCD ring system.</p>

<p>Mucidin is an antifungal antibiotic that inhibits electron transfer reactions within the mitochondrial respiratory chain's cytochrome bc1 complex.</p>

Myxothiazol blocks mitochondrial complex III and triggers SESN2, a gene important for stress response.

Clavicoronic acid, a β-lactamase inhibitor, boosts penicillin antibiotics against resistant bacteria.

<p>MLEB-22043 is a synthetic siderophore-monocyclic β-lactam conjugate which enters bacteria through TonB-dependent transport proteins utilizing its siderophore component, subsequently exerting antibacterial activity via its β-lactam portion. This compound acts as a broad-spectrum antibiotic, exhibiting significant inhibitory activity against pathogens such as Klebsiella pneumoniae, Escherichia coli, Acinetobacter baumannii, and Pseudomonas aeruginosa.</p>

Antifungalagent 113 (compound 9a) serves as an effective antifungal and antibacterial agent. It exhibits strong inhibitory activity against both S. aureus and methicillin-resistant S. aureus.

<p>Cefamandole (lithium), a second-generation broad-spectrum cephalosporin antibiotic, exhibits antimicrobial activity. Upon metabolism in the body, it releases free NMTT, which can lead to hypoprothrombinemia.</p>

<p>Anti-MRSA agent 19 (Compound 1) is an antibiotic that exhibits activity against Staphylococcus aureus. It is active against 40 clinical isolates from the CDC, representing diverse bacterial species with various resistance factors, including resistance to vancomycin, aminoglycoside/tetracycline, and oxazolidinone (median MIC=4 μg/mL).</p>

<p>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.</p>

<p>Ceftolozane TFA is a cephalosporin class antibiotic (antibiotic) designed to inhibit Gram-negative bacterial infections. Additionally, it can be utilized in the synthesis of novel antibiotics (antibiotic) that are more efficacious and safer.</p>

Nikkomycin Z (Nikkomycin Z from Streptomyces tendae) is a competitive chitin synthase inhibitor.It inhibitor of the growth of filamentous fungi, insects,

<p>Bleomycin Free Base, a glycopeptide antibiotic, halts DNA function and treats solid tumors.</p>

<p>Methacycline, a tetracycline antibiotic, inhibits bacterial protein synthesis and effectively suppresses epithelial-mesenchymal transition (EMT). It blocks EMT in vitro and inhibits fibrogenesis in vivo without directly affecting the TGF-β1Smad signaling pathway. As an antimicrobial agent, Methacycline holds potential for research in pulmonary fibrosis.</p>

Ganaplacide hydrochloride (KAF156 HCl) is an orally administered imidazopyrimidine antimalarial agent that inhibits Plasmodium PI4K activity.

Streptonigrin: aminoquinone antibiotic; antitumor, antibacterial; blocks β-Catenin/Tcf, cytotoxic; alters hamster chromosomes; (-)-isomer, CAS#3930-19-6.

Kinamycin B is an antibacterial agent with anticancer activity.

Spicamycin can be used as a potent inducer of differentiation of human myeloid leukemia cells (HL-60) and murine myeloid leukemia cells (M1).

<p>Amicoumacin C is a biological product derived from certain strains of the Bacillus species, specifically fermented by Bacillus subtilis. It is recognized as a potent antibiotic compound, noted for its ability to inhibit bacterial protein synthesis, primarily by interacting with the 30S ribosomal subunit, thereby hindering the translation process.</p>

Sinefungin (Adenosyl-Ornithine) is an effective inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral

Erythromycin and its derivatives; salts thereof

<p>Swainsonine (Tridolgosir) is an alkaloid isolated from Astragalus membranaceus and is a potent and reversible inhibitor of alpha-mannosidase. swainsonine has antitumour activity and induces apoptosis and cell cycle arrest in the G2/M phase.</p>

Formycin A shows antitumor and antiviral activities. Formycin A , a purine nucleoside antibiotic, is a potent human immunodeficiency virus type 1 (HIV-1) inhibitor with an EC50 of 10 μM.

<p>Nortopixantrone(BBR 3438) is a novel 9-azacyclophenanthracene pyrazole that shows antitumor activity in a human prostate cancer model.</p>

<p>A 53868A is an antibiotic, it is isolated from Streptomyces luridus.</p>

Erythromycylamine is a useful organic compound for research related to life sciences. The catalog number is T64443 and the CAS number is 26116-56-3.

<p>Membrane pore-forming agent; H+, K+, Pb2+ ionophore; polyether antibiotic</p>

<p>Cefsulodin sodium salt is a beta lactam antibiotic in the third-generation cephalosporin family that inhibits penicillin-binding proteins (PBPs) to disrupt bacterial cell wall synthesis.</p>

<p>Amicoumacin A is an antibiotic compound, which is derived from the bacterium Bacillus subtilis. This natural source is known for its production of a variety of biologically active compounds that contribute to its utility in numerous scientific contexts. The mode of action of Amicoumacin A involves the inhibition of bacterial protein synthesis by targeting the ribosomal subunit. Specifically, it interferes with the translation process, effectively disrupting the growth and proliferation of susceptible bacterial strains.<br><br>Amicoumacin A is primarily utilized in research settings to study bacterial resistance mechanisms, as well as to explore novel antibacterial therapies. Its application in scientific research extends to examining its potential synergistic effects with other antimicrobial agents, and it serves as a model compound for understanding ribosomal inhibition. The study of Amicoumacin A not only contributes to the broader field of antibiotic development but also offers insights into the molecular interactions that underlie bacterial protein synthesis and antibiotic resistance. This compound's unique properties make it an important subject of investigation for microbiologists and pharmacologists alike, emphasizing its relevance in the ongoing battle against antibiotic-resistant pathogens.</p>

<p>Ticarcillin disodium salt is a beta-lactam antibiotic that has in vitro activity against Gram-positive and Gram-negative bacteria. Ticarcillin is active against penicillinase-producing strains of Staphylococcus aureus, Enterobacter aerogenes, Proteus mirabilis, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Serratia marcescens, Streptococcus pyogenes, Streptococcus faecalis, and Streptococcus pneumoniae. Furthermore, it inhibits transpeptidase activity of the cell wall of bacteria which prevents peptidoglycan synthesis. It is bactericidal for many bacteria at low concentrations.</p>

<p>Tobramycin is used to treat severe infections with gram-negative bacteria and it is often applied in combination with beta-lactams. It has similar antimicrobial effects to gentamicin and is effective against all Enterobacteriacae, but more effective than gentamicin against P. aeruginosa, which is why it is often used for gentamicin-resistant strains, especially in the case of cystic fibrosis.</p>

<p>Potassium clavulanate is a beta-lactamase inhibitor and an antibacterial agent. The presence of potassium clavulanate in culture media inhibits the activity of beta-lactamases, which are enzymes that confer resistance to penicillin and other beta-lactam antibiotics. It also has been shown to be active against bacterial infections such as tuberculosis, sepsis, and pneumonia, where it can inhibit the growth of bacteria by interfering with their ability to form cell walls. Potassium clavulanate is also used as an antimicrobial agent for blood culture technique and antimicrobial treatment.</p>

PKUMDL-LTQ-301 is a potent inhibitor of HipA toxin. PKUMDL-LTQ-301 also inhibits E. coli persistence.

<p>DprE1-IN-8 is a potent inhibitor of DprE1, exhibiting an IC50 of less than 0.75 μM.</p>