Antibiotiques

Membrane-disrupting agent

Maduramicin ammonium is an anticoccidial agent with action on protozoal parasites by disrupting ion gradients and is used for preventing coccidiosis in poultry.

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.

Pazufloxacin hydrochloride is a synthetic antibacterial agent, which is derived from the fluoroquinolone class of antibiotics with a broad-spectrum activity against various bacterial pathogens. This compound, sourced through chemical synthesis, functions primarily by inhibiting bacterial DNA gyrase and topoisomerase IV, which are critical enzymes for DNA replication, transcription, repair, and recombination. The inhibition of these enzymes leads to the disruption of bacterial DNA processes, ultimately resulting in bacterial cell death.

Inhibitor of protein synthesis; streptogramin

Carbomycin is a macrolide antibiotic, which is derived from the bacterium Streptomyces halstedii. This antibiotic functions by binding to the 50S ribosomal subunit, thereby inhibiting bacterial protein synthesis. Through this mechanism, carbomycin effectively disrupts the growth and replication of susceptible bacterial strains, making it a potent tool in combating bacterial infections.

Ampicillin is a β-lactam antibiotic with a broad spectrum of activity against Gram-positive and Gram-negative bacteria. It is used in the treatment of bacterial infections, including those caused by methicillin-resistant Staphylococcus aureus (MRSA), Streptococcus pneumoniae, and Listeria monocytogenes. Ampicillin binds to penicillin-binding proteins in the bacterial cell wall by competitive inhibition. It prevents the formation of an antibiotic-inhibitor complex with the enzyme cell wall synthesis that is required for cell wall biosynthesis, inhibiting protein synthesis and cell division.

Methacycline HCl is a tetracycline antibiotic with action on bacterial protein synthesis by binding to the 30S ribosomal subunit and is used for treating bacterial infections such as respiratory and urinary tract infections.

9-Erythromycin 9-oxime is an activty inpurity, binding to the 50S ribosomal subunit of bacteria.

Inhibitor of inosine monophosphate dehydrogenase; immunosuppressant

Monensin sodium is a polyether antibiotic with action on ion transport across bacterial cell membranes and is used for preventing coccidiosis and improving feed efficiency in livestock.

Neomycin, one of the many oligosaccharide containing antibiotics, is an aminoglycoside antibiotic found in Streptomyces fradiae (Collins, 2006) with wide spectrum, active against Gram-negative Gram-positive bacteria. Neomycin is commony used as a selection marker in cloning, and is therefore used in growth media to select colonies with the neomycin resistance cassette integrated into their genome. Neomycin is a mixture of neomycin B (Framycetin) and its epimer Neomycin C, the latter component accounting for some 5–15% of the mixture.

Fluoroquinolone; gyrase inhibitor

Novobiocin is an aminocoumarin antibiotic with action on bacterial DNA gyrase to inhibit ATPase activity and is used for treating staphylococcal infections and research on DNA replication.

Olaquindox is a quinoxaline derivative antibiotic with action on bacterial growth suppression in the gut and is used for promoting growth and controlling bacterial infections in livestock.

Rifapentine is a rifamycin antibiotic with action on bacterial RNA polymerase to inhibit transcription and is used for treating active and latent tuberculosis.

Inhibits chaperone protein HSP90; anti-proliferative; antineoplastic

Inhibitor of isoleucyl-tRNA synthetase; inhibitor of protein synthesis

Kanamycin sulfate is a water-soluble antibiotic. Genes encoding kanamycin resistance are commonly used as selection markers in molecular biology .It acts during the translation mechanism in prokaryotic ribosomes to avoid bacterial cell growth.

Pefloxacin mesylate is a fluoroquinolone antibiotic with action on bacterial DNA gyrase and topoisomerase IV and is used for treating bacterial infections, including urinary and respiratory tract infections.

Inhibitor of protein synthesis; aminoglycoside

Validamycin A is an antibiotic and fungicide with action as a trehalase inhibitor, disrupting carbohydrate metabolism in fungi and is used for controlling fungal diseases like sheath blight in rice and damping-off in cucumbers.

Puromycin is active against both prokaryotic and eukaryotic cells. Puromycin resistance gene (pac) is a common choice for the selection of mammalian cells since its first application in 1988, especially for therapeutic proteins in mammalian cells where it was used to produce high levels of protein of interest. Puromycin can also be used as a selection marker for Archea.

Inhibitor of protein synthesis; aminoglycoside

Lincomycin is active against gram-positive bacteria such as staphylococci, streptococci, pneumococci, diphtheria bacillus, and clostridia. It is used to treat severe bacterial infections including: sepsis, osteomyelitis, septic endocarditis, pneumonia, pulmonary abscess, infected wounds, purulent meningitis and severe pseudomembranous colitis. Lincomycin is an alternative antibiotic for penicillin-resistant gram-positive bacteria.

Isepamicin sulfate - 70% is a semi-synthetic aminoglycoside antibiotic, which is derived from naturally occurring antibiotic compounds through chemical modifications. Its mode of action involves binding to the bacterial 30S ribosomal subunit, disrupting protein synthesis and consequently causing bacterial cell death. This mechanism of action is typical of aminoglycosides, characterized by their bactericidal properties against a broad spectrum of Gram-negative bacteria, with some efficacy against certain Gram-positive bacterial strains.

Sulopenem is a thiopenem antibiotic with action on bacterial cell wall synthesis and is used for treating uncomplicated urinary tract infections.

Sulfadoxine is a long-acting sulfonamide antibiotic with action on bacterial folate synthesis inhibition and is used for treating malaria in combination with pyrimethamine.

Ionomycin calcium is a potent calcium ionophore, which is derived from natural sources such as certain Streptomyces species. Its primary mode of action involves facilitating the translocation of calcium ions (Ca^2+) across biological membranes, specifically transporting them from external environments or intracellular stores into the cytoplasm. This action significantly elevates intracellular calcium levels.

Sitafloxacin is an antibacterial agent belonging to the fluoroquinolone class of antibiotics, which is synthetically derived from chemical processes involving fluorinated quinolones. Its mode of action involves the inhibition of bacterial DNA gyrase and topoisomerase IV, enzymes crucial for bacterial DNA replication and transcription. By interfering with these enzymes, Sitafloxacin effectively hampers bacterial DNA synthesis, leading to the eventual demise of the bacterial cell.

Aminosidine is a nucleoside analogue that inhibits the HIV-1 reverse transcriptase and the integrase, which are enzymes involved in viral DNA synthesis. Aminosidine is active against Leishmania spp., but not against bacteria. Aminosidine has been shown to be effective in experimental models of human bowel disease and in patients with inflammatory bowel disease. It was also found to be active against wild-type strains of human immunodeficiency virus type 1, but not resistant mutants. The mechanism of action is the inhibition of cellular mitochondrial membrane potential.

Tyrothricin is a peptide antibiotic, which is derived from the bacterium Bacillus brevis. This compound comprises a mixture of polypeptides, primarily gramicidin and tyrocidine, both of which are instrumental in its antimicrobial activity. The mode of action of tyrothricin involves disrupting bacterial cell membranes, leading to cell lysis and death. Gramicidin increases the permeability of the bacterial membrane to ions, while tyrocidine promotes disruption of membrane integrity, which together exert bactericidal and bacteriostatic effects.

Telavancin is a lipoglycopeptide antibiotic, which is a semi-synthetic derivative of vancomycin. Its source is derived through modifications of the glycopeptide antibiotic, specifically aimed to enhance antibacterial activity. Telavancin functions by inhibiting cell wall synthesis in Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA). It does this by binding to the D-alanyl-D-alanine terminus of cell wall precursors, disrupting peptidoglycan polymerization and, consequently, cell wall integrity. Additionally, Telavancin increases membrane permeability and disrupts membrane potential, further enhancing its bactericidal activity.

26-Oxofusidic acid is a derivative of fusidic acid, which is a potent antibacterial compound originally isolated from the fungus Fusidium coccineum. This compound exhibits a unique mode of action by inhibiting bacterial protein synthesis through interference with the elongation factor G (EF-G), a critical component in the translocation step of translation. By targeting this specific aspect of bacterial metabolism, 26-Oxofusidic acid effectively disrupts the growth of gram-positive bacteria, making it an invaluable tool in combating resistant bacterial strains.

Piperacillin oxalylamide is an investigational antibiotic, which is a synthetic derivative of the widely used β-lactam antibiotic, piperacillin. Its development is rooted in the quest to combat β-lactamase-producing resistant bacterial strains, which are a growing threat in clinical settings. It operates by inhibiting bacterial cell wall synthesis, similar to other β-lactam antibiotics, but possesses a modified structure that enhances its resistance to enzymatic degradation by β-lactamases.

Cefquinome sulfate is a cephalosporin antibiotic, which is a synthetic, broad-spectrum antimicrobial agent. It is derived from the beta-lactam family, specifically designed to combat Gram-positive and Gram-negative bacterial pathogens. The mode of action involves inhibiting bacterial cell wall synthesis. It achieves this by binding to penicillin-binding proteins (PBPs) within the bacterial cell wall, ultimately leading to cell lysis and death due to the interruption of necessary cell wall components.

Dicloxacillin is a penicillin antibiotic that is used to treat bacterial infections of the gastrointestinal tract, skin, and urinary tract. It binds to the penicillin-binding proteins in bacterial cell walls by competitive inhibition. Dicloxacillin inhibits bacterial growth by binding to the enzyme cell wall synthesis that is required for cell wall biosynthesis, inhibiting protein synthesis and cell division. This drug also has a toxic effect on respiratory system cells, which may be due to its ability to induce apoptosis. Dicloxacillin sodium salt is available as tablets for oral administration or as an intravenous solution for injection. It can interact with other drugs, such as benzalkonium chloride and matrix effect; it also has analytical methods such as chromatographic analysis and rate constant.

Borrelidin is a potent antibiotic of the polyketide class, which is isolated from various Streptomyces species. Its mode of action is characterized by its inhibition of threonyl-tRNA synthetase, effectively disrupting protein synthesis within bacteria. Additionally, Borrelidin is known for its unique anti-angiogenic properties, which result from the inhibition of endothelial cell proliferation, making it a compound of interest in cancer research.

Pazufloxacin is an antibacterial agent, which is a synthetic derivative originating from the fluoroquinolone class of compounds. This source categorizes it alongside a group of broad-spectrum antibiotics known for their efficacy against a wide variety of bacterial pathogens. The mode of action of pazufloxacin involves the inhibition of bacterial DNA gyrase and topoisomerase IV. These are essential enzymes for bacterial DNA replication, transcription, repair, and recombination processes. By inhibiting these enzymes, pazufloxacin disrupts the bacterial DNA processes, ultimately leading to cell death.

Phleomycin is an antibiotic, which is derived from the bacterium *Streptomyces verticillus*. Its mode of action involves binding to DNA and inducing breaks by generating free radicals in the presence of oxygen and ferrous ions, leading to cell death. Phleomycin is prominently used in molecular biology applications as a selective agent in the generation of stable transfectants. It is particularly effective in selecting for cells that have integrated vectors conferring resistance, such as the Sh ble gene used in yeast, plant, and mammalian cell systems. Due to its potent DNA-cleaving ability, Phleomycin is valuable in studies requiring stringent selection pressure. Researchers commonly utilize it in experiments focusing on genetic modification and cellular resistance development.

Mitomycin C analogue

N'-Desmethyl azithromycin is a semi-synthetic derivative antibiotic, which is derived from the chemical modification of azithromycin, a macrolide antibiotic sourced originally from the bacterium *Streptomyces erythreus*. It functions primarily by inhibiting bacterial protein synthesis, binding specifically to the 50S ribosomal subunit, which results in the prevention of transpeptidation and translocation processes during translation. This action effectively halts bacterial growth, rendering it bacteriostatic.

Ionomycin is an ionophore compound with a mode of action that facilitates calcium ion transport across cell membranes. It is used in research to study calcium signaling and T-cell activation.

Nigericin transports cations across the membrane of the cell and it is used to study anion transport. It can be used as a buffer to control pH value inside of the cell.

Oligomycin B is an antibiotic compound, which is derived from Streptomyces species. It is an inhibitor of the mitochondrial ATP synthase complex, specifically targeting the F₀ subunit of ATP synthase. This action obstructs the proton channel, preventing the flow of protons across the mitochondrial membrane. As a result, Oligomycin B effectively halts ATP synthesis by oxidative phosphorylation, which is crucial for the survival of aerobic organisms.

PNU 142300 is a non-peptidyl anticoagulant, which is a synthetically derived small molecule. This compound is sourced from advanced chemical synthesis techniques that focus on mimicking biological activity through non-biological materials. PNU 142300 acts by specifically inhibiting factor Xa, a crucial enzyme in the coagulation cascade responsible for the conversion of prothrombin to thrombin. By targeting this enzyme, it effectively prevents the formation of blood clots, thereby exhibiting potent anticoagulant properties.

Inhibitor of protein synthesis; glycylcycline class

Thienamycin is a β-lactam antibiotic, which originates from the fermentation of the bacterium *Streptomyces cattleya*. Its mode of action involves inhibiting the synthesis of bacterial cell walls. Thienamycin accomplishes this by binding to penicillin-binding proteins (PBPs) critical for peptidoglycan construction, thereby disrupting cell wall integrity and leading to bacterial lysis.

(E)-10,11-Didehydro-11-deoxy-6-O-methylerythromycin is a semisynthetic macrolide antibiotic, which is derived from erythromycin, a natural product obtained from the bacterium *Saccharopolyspora erythraea*. This compound functions as an inhibitor of protein synthesis by binding to the 50S ribosomal subunit of bacteria, thus preventing the growth and proliferation of susceptible bacterial strains. The alteration in its chemical structure, notably the methylation at the 6-O position, enhances its stability and improves its pharmacokinetic profile compared to the parent compound, erythromycin.

Cefquinome is a broad-spectrum antibiotic, which is a fourth-generation cephalosporin. It is derived from the β-lactam class of antibiotics and is specifically designed for veterinary applications. Its mode of action involves the inhibition of bacterial cell wall synthesis, leading to cell lysis and death. This action is facilitated through the binding of cefquinome to penicillin-binding proteins, which undermines the structural integrity of bacterial cell walls, proving effective against both Gram-positive and Gram-negative bacteria.

Oxacillin sodium is a beta-lactam antibiotic with action on bacterial cell wall synthesis and is used for treating infections caused by penicillin-resistant Staphylococcus aureus.

N-Biotinyl-12-aminododecanoyltobramycin amide is a synthetic bioconjugate, which is derived from the aminoglycoside antibiotic tobramycin. This compound is chemically modified by the addition of a biotin moiety linked through a 12-aminododecanoyl spacer. The source of this product is rooted in the conjugation of biotin to tobramycin, allowing for targeted delivery and potential hybrid applications in both therapeutic and diagnostic fields.

Virginiamycin - Complex of M1+S1 is an antibiotic compound, which is derived from the actinobacterium Streptomyces virginiae. It functions through the inhibition of bacterial protein synthesis by binding to the 50S ribosomal subunit, thereby obstructing peptide bond formation and impeding microbial growth. The complex is composed of two major components: Virginiamycin M1 and Virginiamycin S1, which synergistically enhance antimicrobial efficacy.

Nonactin is a macrotetrolide antibiotic with action as an ionophore for potassium and ammonium ions and is used for research on ion transport and bacterial inhibition.

Metabolite of rifampicin

Pirlimycin HCl is an antibacterial product, which is a semi-synthetic derivative of the natural antibiotic lincomycin produced by Streptomyces lincolnensis. Its mode of action involves the inhibition of bacterial protein synthesis by binding to the 50S ribosomal subunit, thereby preventing the elongation of peptide chains. This action is particularly effective against Gram-positive bacteria, including Staphylococcus and Streptococcus species.

Polymyxin B nonapeptide hydrochloride is a potent antibiotic compound derived from the bacterium *Bacillus polymyxa*. As a cationic polypeptide, it exhibits its antibacterial activity by interacting with the lipopolysaccharides and phospholipids in the bacterial cell membrane, leading to increased permeability and ultimately causing cell lysis. The compound is specifically effective against a broad range of Gram-negative bacteria, making it crucial in studying antibiotic resistance mechanisms.

Sarecycline is a tetracycline-class antibiotic, which is derived from naturally occurring tetracycline antibiotics. Its mode of action involves inhibition of bacterial protein synthesis by binding to the 30S ribosomal subunit, thereby preventing the addition of amino acids to nascent peptide chains. This specific mechanism disrupts bacterial growth, making Sarecycline effective against certain strains of bacteria implicated in dermatological conditions.

8-Fluoro erythromycin is a synthetic derivative of the macrolide antibiotic erythromycin. It is derived from the fermentation of *Streptomyces erythraeus*, a species known for producing erythromycin, which is chemically modified to include a fluorine atom at the eighth position. This modification enhances its pharmacokinetic properties, improving its stability and bioavailability compared to the parent compound.

Gentamicin C2 pentaacetate (2 : 1 Mixture of C2 and C2a) is an aminoglycoside class antibiotic derivative, primarily derived from the fermentation of Micromonospora species. This product is a semi-synthetic compound, combining two closely related gentamicin components, C2 and C2a, in a specified ratio. Its mode of action involves binding to the 30S subunit of the bacterial ribosome, which disrupts protein synthesis resulting in bactericidal activity against a wide spectrum of Gram-negative and some Gram-positive bacteria.

Cefotiam is a broad-spectrum cephalosporin antibiotic, which is a beta-lactam compound derived from the mold Acremonium. It functions by inhibiting bacterial cell wall synthesis, particularly by targeting penicillin-binding proteins, which leads to cell lysis and death in susceptible bacteria. This mechanism of action makes it effective against various Gram-positive and Gram-negative bacteria.

Porfiromycin is an antineoplastic antibiotic with action on DNA alkylation and cross-linking and is used for research on cancer treatment, particularly for hypoxic tumors.

Tridehydro pirlimycin is an antibiotic compound, which is a synthetic derivative with origins in the lincosamide family. It is characterized by its ability to inhibit bacterial protein synthesis by binding to the 50S ribosomal subunit, leading to a bacteriostatic effect. The compound is primarily developed for its use in veterinary medicine, particularly in the treatment and management of bacterial infections in animals.

Tropodithietic acid is a bioactive compound, which is a potent antibacterial agent derived from certain marine bacteria, including the genus Phaeobacter. This antibiotic is characterized by its ability to disrupt quorum sensing, a mechanism that bacteria use for communication and coordination of group behaviors, including virulence. By interfering with this process, tropodithietic acid impedes bacterial colonization and biofilm formation, effectively inhibiting pathogenic activity.

Cefodizime is a third-generation cephalosporin antibiotic, which is derived from the fungus Acremonium. It exerts its bactericidal effects by inhibiting bacterial cell wall synthesis. This action is achieved through binding to penicillin-binding proteins (PBPs), leading to the interruption of peptidoglycan cross-linking essential for the bacterial cell wall integrity. The breakdown of cell wall synthesis results in the lysis and death of the bacterial cell.

Piericidin A is a microbial metabolite, specifically a type of polyketide, which is derived from the bacterium of the genus Streptomyces. This compound acts as an electron transport chain inhibitor by specifically binding to the ubiquinone binding site of complex I (NADH:ubiquinone oxidoreductase) in mitochondria. This mode of action results in the disruption of ATP production through oxidative phosphorylation.

Lydicamycin is an antibacterial compound, which is a polyketide-derived antibiotic produced by the microorganism Streptomyces. This natural compound functions by inhibiting bacterial protein synthesis, effectively interrupting critical cellular processes within susceptible bacteria. The mode of action primarily focuses on binding to the bacterial ribosome, thereby disrupting protein production and inhibiting bacterial growth.

Exhibits antitumour activity against L1210 and P388 leukemias and B16 melanoma

PC 190723 is a synthetic chemical compound, which is derived through targeted chemical synthesis processes involving precise organic reactions. Its mode of action involves disrupting cellular division by inhibiting specific protein functions essential for the mitotic process. This molecular interaction results in potent effects on cell division, making it a valuable tool for studying cellular mechanics and developing therapeutic strategies.

10, 11-Dehydrocurvularin is a fungal phytotoxin with heat shock response and immune-modulatory activitie. Curvularins inhibit the expression of the inducible nitric oxide synthase (iNOS), thereby acting as anti-inflammatory agents and immune system modulators

Trovafloxacin mesylate is a synthetic antibiotic belonging to the fluoroquinolone class, which is derived from chemical synthesis processes rather than natural sources. The mode of action of trovafloxacin mesylate involves the inhibition of bacterial enzymes DNA gyrase and topoisomerase IV. These enzymes are essential for DNA replication, repair, and transcription within the bacterial cell. By inhibiting these enzymes, trovafloxacin mesylate disrupts bacterial DNA processes, leading to cell death and exerting its antibacterial effects.

Vancomycin aglycon is a glycopeptide antibiotic, which is a derivative of vancomycin. It is sourced from the fermentation products of certain Amycolatopsis species, a genus of actinobacteria. The mode of action of vancomycin aglycon involves the inhibition of bacterial cell wall synthesis. It specifically binds to the D-Ala-D-Ala terminus of nascent peptidoglycan chains, thereby preventing the cross-linking that is crucial for maintaining cell wall integrity.

A macrolide, broad-spectrum antibiotic that targets cytochrome P4503A4 (CYP3A4). Clarithromycin has been used to potentiate the pharmacological effects of some drugs that are metabolised by the cytochrome P450.

Clarithromycin-13CD3 is an isotopically labeled macrolide antibiotic, which is synthesized to include deuterium (D) and carbon-13 (^13C) in its molecular structure. This modified compound serves as a stable isotope-labeled standard, primarily sourced from chemical synthesis. The incorporation of these isotopes differentiates it from the naturally occurring antibiotic, enabling its use in precise analytical studies.

Narasin is an ionophore antibiotic, which is a fermentation product derived from certain strains of the bacterium *Streptomyces aureofaciens*. It functions by disrupting the ion gradients across cell membranes, specifically facilitating the transport of sodium and potassium ions. This action interferes with the energy metabolism of certain pathogenic microorganisms, rendering them unable to proliferate effectively.