Antimicrobials

<p>Streptomycin sulfate is an antibiotic that inhibits the growth of bacteria by binding to the ribosomal subunit and interfering with protein synthesis. It is used in culture media for the production of human antibodies as well as in drug therapy for methicillin-resistant staphylococcus. Streptomycin sulfate has a high specific activity and low sensitivity, but it also has a low solubility in water. The active form of streptomycin sulfate is streptomycin A, which is produced by the addition of a phenyl ring to neomycin sulfate. In plant roots, streptomycin sulfate inhibits cyanogenic glycosides from being hydrolyzed into hydrogen cyanide (HCN) and benzaldehyde.</p>

<p>Aminoglycoside antibiotic; inhibits protein synthesis by inducing miscoding</p>

<p>Inhibitor of protein synthesis; steroid antibiotic</p>

<p>Ganciclovir is an acyclovir analog that is used in the treatment of cytomegalovirus and herpetic keratitis of the eye. This drug is a DNA polymerase inhibitor and exhibits its anti-viral properties by inhibiting viral replication.</p>

<p>Amphotericin B is a macrocycle antibiotic first isolated from Streptomyces nodosus. Its antifungal activity is exerted by interacting with the fungal membrane, mainly ergosterol, and inducing pore formation. The increase in membrane permeability causes loss of ions and cell death. The C-2’ hydroxyl residue of the mycosamine carbohydrate moiety in the structure seems to have a major role in binding to ergosterol. It is used in cell culture to prevent growth of microbial contaminants, such as yeast and fungi. It is recommended by the WHO and CDC as an antifungal component for VTM at a concentration of 250ug/ml.</p>

<p>2-Methyl-4-isothiazolin-3-one HCl , also known as MIT hydrochloride is often used as a preservative in personal care products and other industrial applications. The product has shown to act as an antimicrobial and antifungal agent.</p>

<p>Posaconazole is an antifungal agent that inhibits the 14-alpha demethylase enzyme which is responsible for the synthesis of the fungal cell wall component, ergosterol. This demethylase enzyme synthesizes ergosterol through converting lanosterol to ergosterol. Therefore Posaconazole prevents the formation of fungal cell walls with the appropriate membrane permeability thus leading to fungal cell lysis. Posaconazole can be used as an antifungal drug to treat opportunistic fungal infections in immunocompromised individuals such as HIV patients. Moreover it is shown to inflict its inhibitory activity against common pathogenic fungus such as Candida and Aspergillus species but also Mucorales and some Fusarium species, which are less common.</p>

<p>Inhibitor of beta-lactamase; inhibitor of cell wall synthesis; beta-lactam class</p>

<p>Erythromycin thiocyanate is a macrolide antibiotic derivative with action on bacterial protein synthesis inhibition and is used for research and pharmaceutical applications.</p>

<p>A broad-spectrum antibiotic of tetracycline class which inhibits protein synthesis by targeting the 30S ribosome subunit. It has been used in human medicine as well as in veterinary medicine and agriculture.</p>

<p>Atazanavir is a HIV-1 protease inhibitor, used in the anti-retroviral therapy of adult and sometimes paediatric patients infected with HIV. In in vitro studies with human pulmonary epithelial cells, atazanavir has been studied as a potential inhibitor of SARS-CoV-2 Mpro protease, with the aim of halting viral replication.</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>Anthracycline antibiotic with potent anti-tumoral activity. The compound interferes with DNA replication and RNA transcription since it intercalates between the base pairs of nucleic acids. It also inhibits the topoisomerase II, proteasome and generates free radicals, which leads to cell death of treated cells. Moreover, daunorubicin triggers apoptosis trough the stimulation of ceramide synthesis. It has been used as chemotherapy agent for the treatment of myeloid leukaemia (AML) and acute lymphocytic leukaemia (ALL).</p>

<p>Piperacillin sodium is a broad-spectrum beta-lactam antibiotic with action on bacterial cell wall synthesis and is used for treating severe infections caused by gram-negative bacteria, including Pseudomonas aeruginosa.</p>

<p>Tenofovir disoproxil is a nucleotide analog reverse transcriptase inhibitor that is used to treat infections such as Hepatitis-B and HIV. This drug is an antiretroviral agent that blocks reverse transcriptase, blocking viral replication.</p>

<p>STAADIUM™ PhosphoZide is a targeted inhibitor of phosphatase-producing bacteria, which is activated by phosphatase itself. STAADIUM™ PhosphoZide targets specifically methicillin-resistant Staphylococcus aureus (MRSA) and its antibacterial activity is triggered by both the acid and alkaline phosphatases that the bacteria produce. STAADIUM™ PhosphoZide can be added as an enzyme-specific selective supplement to agar plates or as an enrichment agent to a broth culture. More details in the application notes document.</p>

<p>Amorolfine is an antifungal drug that inhibits fungal enzymes (D14 reductase and D7-D8 isomerase). Its inhibition has an affect on fungal sterol synthesis pathways, and it depletes ergosterol. This drug can be used as a treatment for inflammatory lesions such as Tinea corporis, Tinea pedis, and Tinea cruris due to its ability to penetrate the skin barrier with ease.</p>

<p>Fungicide</p>

<p>Torezolid (Tedizolid) is an oxazolidinone antibiotic with action on bacterial protein synthesis by binding to the 50S ribosomal subunit and is used for treating acute bacterial skin and skin structure infections.</p>

<p>Tolnaftate is a thiocarbamate antifungal agent with action on fungal cell membrane disruption and is used for treating fungal infections like athlete's foot, jock itch, and ringworm.</p>

<p>Anthelmintic; inhibitor of tubulin polymerization</p>

<p>Netropsin dihydrochloride is a pyrrole-amidine antibiotic with action on AT-rich sequences of DNA to inhibit replication and is used for research on DNA-binding properties and antiviral activity.</p>

<p>Ticarcillin is a beta-lactam antibiotic that inhibits the synthesis of peptidoglycan, which is an essential component of bacterial cell walls. Ticarcillin is used for the treatment of infections caused by susceptible bacteria, such as those in the respiratory tract, urinary tract, skin and soft tissues. It can also be used to treat sepsis and meningitis. Ticarcillin has a broad spectrum of activity against Gram-positive and Gram-negative bacteria, including Enterobacteriaceae (e.g., Escherichia coli) and Pseudomonas aeruginosa. Ticarcillin is not active against methicillin-resistant Staphylococcus aureus (MRSA).</p>

<p>Cefpodoxime proxetil is a prodrug of cefpodoxime with action on bacterial cell wall synthesis and is used for treating bacterial infections such as pneumonia, bronchitis, and gonorrhea.</p>

<p>Natural diterpene; anti-microbial</p>

<p>Boceprevir is a peptidomimetic, covalent inhibitor of NS3/4A serine protease from hepatitis C virus (HCV). Boceprevir also inhibits and acts as a substrate in the cytochrome P450 3A4 (CYP3A) metabolic pathway. Boceprevir was recently shown to inhibit the main protease Mpro (3CLpro) from SARS-CoV-2 with IC50 of 4.13 μM and EC50 of 1.31 μM.</p>

<p>Gamithromycin is a macrolide antibiotic with action on bacterial protein synthesis and is used for treating respiratory infections in cattle, pigs, and sheep.</p>

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

<p>Dihydrostreptomycin sesquisulfate, EP is an aminoglycoside antibiotic, structurally derived from Streptomyces griseus. This compound originates from microbial biosynthesis, a method which harnesses the natural antibiotic-producing capabilities of microbial cultures. The mode of action of dihydrostreptomycin sesquisulfate involves binding to the 30S subunit of bacterial ribosomes, which interrupts the process of protein synthesis, ultimately leading to bacterial cell death.</p>

<p>A fluoroquinolone antibiotic which inhibits nucleic acid synthesis by targeting the DNA gyrase and topoisomerase IV. This second-generation fluoroquinolone has a broad spectrum of action and is more effective against Gram-negative bacteria.</p>

<p>Pimodivir is a non-nucleoside-derived inhibitor of the polymerase basic protein 2 (PB2) subunit found in the polymerase complex of the influenza A virus. In general, pimodivir is indicated for the treatment of patients with severe influenza although knowledge about possible rise of resistance is not available.</p>

<p>Temocillin disodium is a beta-lactamase-resistant penicillin antibiotic with action on bacterial cell wall synthesis and is used for treating infections caused by multidrug-resistant gram-negative bacteria.</p>

<p>Inhibitor of protein synthesis; aminocyclitol class</p>

<p>Epioxytetracycline is a degradation product of the antibiotic oxytetracycline. It has been found in wastewater.</p>

<p>Doxorubicin (DOX) is an antineoplastic chemotherapy drug used to treat breast, ovarian and pancreatic cancers. It is an antitumor antibiotic that inhibits DNA topoisomerase II. DOX interferes with the topoisomerase II-mediated repair of DNA causing accumulation of mutations. It also leads to the generation of reactive oxygen species (ROS), which further damage DNA as well as proteins and membranes. However, the compound presents with a risk of developing cardiomyopathy as well as drug resistance. Pegylated liposomal doxorubicin has also been developed to treat breast and ovarian cancers, myeloma, and HIV-related Kaposi’s sarcoma.</p>

<p>Cefotaxime sodium is a broad-spectrum cephalosporin antibiotic, which is a semisynthetic derivative of cephalosporin C obtained from the mold Acremonium. This compound functions by inhibiting bacterial cell wall synthesis, which it achieves through binding to and deactivating penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. This action prevents the cross-linking of peptidoglycan chains, leading to cell lysis and bacterial death, primarily affecting rapidly dividing cells.</p>

<p>Ipconazole is a fungicide with a mode of action that inhibits ergosterol biosynthesis, disrupting fungal cell membranes. It is used for seed treatment to protect crops like cereals and vegetables from fungal diseases. It's sold as a mixture of two isomers.</p>

<p>Inhibits chaperone protein HSP90; anti-proliferative; antineoplastic</p>

<p>Broad-spectrum antibiotic; bacterial cell wall biogenesis inhibitor</p>

<p>Anti-fungal; glucan synthase inhibitor</p>

<p>STAADIUM™ PeptiZide L-Ala is a targeted inhibitor for L-alanine aminopeptidase-producing bacteria. The antibacterial activity of STAADIUM™ PeptiZide L-Ala is triggered by the enzyme L-alanine aminopeptidase, an enzyme located in the bacterial cell wall and is a characteristic of Gram-negative bacteria. L-alanine aminopeptidase has not been experimentally detected in Campylobacter species, anaerobic bacilli, Gram-positive and Gram-variable bacteria. More details in the application notes document.</p>

<p>Flubendazole is a benzimidazole anthelmintic with action on microtubule formation in parasites and is used for treating intestinal worms in humans and animals.</p>

<p>Inhibitor of cell wall biogenesis; glycopeptide antibiotic</p>

<p>Antibiotic of tetracycline class; protein synthesis inhibitor</p>

<p>Tetracycline is a broad-spectrum antibiotic that is effective against a variety of bacterial infections. It is a polyketide antibiotic that inhibits protein synthesis by binding to ribosomes and preventing the attachment of amino acids to tRNA molecules thus inhibiting bacterial growth.</p>

<p>Anti-retroviral; HIV protease inhibitor</p>

<p>Inhibits DNA gyrase and topoisomerase IV</p>

<p>Difloxacin is a fluoroquinolone antibiotic, which is a synthetic compound derived from chemical synthesis methods. Its source involves complex organic chemistry that modifies the quinolone backbone to enhance its antibacterial properties. Difloxacin functions by inhibiting bacterial DNA gyrase and topoisomerase IV, which are critical enzymes involved in DNA replication, transcription, and repair. This inhibition leads to the prevention of cellular division and ultimately results in bacterial cell death.</p>

<p>Inhibitor of DNA replication; aminoglycoside class</p>

<p>Ketoconazole is an azole antifungal compound with a mode of action that inhibits ergosterol synthesis, disrupting fungal cell membranes. It is used for treating fungal infections of the skin and scalp.</p>

<p>Cefadroxil is a first-generation cephalosporin antibiotic with action on bacterial cell wall synthesis and is used for treating infections like strep throat, skin infections, and urinary tract infections.</p>

<p>Tomopenem is a carbapenem antibiotic, which is a product of synthetic origin with broad-spectrum antibacterial properties. It acts by inhibiting the synthesis of bacterial cell walls through binding to penicillin-binding proteins, thereby disrupting the structural integrity of the cell wall and leading to bacterial cell lysis and death.</p>

<p>Mebendazole is a benzimidazole anthelmintic with action on microtubule formation in parasitic worms and is used for treating intestinal worm infections like threadworms and roundworms.</p>

<p>Nevirapine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with action on HIV reverse transcriptase to block viral replication and is used for treating HIV/AIDS in combination therapies.</p>

<p>A broad-spectrum antibiotic of macrolide class, which targets 50S ribosomal subunit and inhibits protein synthesis. Erythromycin is widely used in molecular biology and biotechnology as a selection marker. Erythromycin is also an agonist of the motilin receptor, and it has prokinetic activity on the gut.</p>

<p>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.</p>

<p>N-Demethyl roxithromycin is a metabolite of roxithromycin with action on bacterial protein synthesis inhibition and is used for research on macrolide antibiotics.</p>

<p>Cefatrizine propylene glycol is a cephalosporin antibiotic with action against gram-positive and gram-negative bacteria and is used for treating respiratory and skin infections.</p>

<p>Broad-spectrum fluoroquinolone antibacterial agent</p>

<p>Cefepime dihydrochloride monohydrate is a fourth-generation cephalosporin antibiotic with action on bacterial cell wall synthesis and is used for treating severe bacterial infections, including pneumonia and urinary tract infections.</p>

<p>Inhibitor of hepatitis C viral enzyme NS3-4A serine protease</p>

<p>Repromicin is a novel antibiotic, which is derived from a unique strain of actinobacteria. This organism is known for its ability to produce a wide range of bioactive compounds. Repromicin operates by inhibiting bacterial protein synthesis, a mode of action that involves binding to the bacterial ribosome and interfering with the translation process. This leads to an effective halt in bacterial growth and proliferation.</p>

<p>Baloxavir marboxil is a selective inhibitor of the cap-dependent endonuclease of RNA polymerase, an acidic protein in influenza A and B viruses. In patients, baloxavir marboxil reduces the time to recovery by alleviating the symptoms of the influenza A and B infection, in both adults and children.</p>

<p>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.</p>

<p>Cefpodoxime is a semi-synthetic antibiotic that is clinically used against bacterial infections. The chemical structure of Cefpodoxime is similar to Cephalexin and has high bioavailability and high resistance to inhibit bacterial growth. Cefpodoxime acts inhibiting the synthesis of cell wall, the cross-linking of peptidoglycan and altering bacterial permeability by inhibiting lipopolysaccharide synthesis. Studies have shown that cefpodoxime can be used for treating prophylaxis of respiratory tract infections, in which being absorbed from the gastrointestinal tract unchanged and is metabolized to an active form in liver cells both after oral ingestion or after a single parenteral dose.</p>

<p>Inhibitor of protein synthesis; aminoglycoside</p>

<p>Selective and potent inhibitor of sialidases (neuraminidases) in influenza A and B viruses. The compound binds tightly to the viral neuraminidase active site in late stages of viral life-cycle. It inhibits shedding sialic acids from host cell surface glycans, which interact with viral hemagglutinin, and consequently prevents release of new viral particles from the host cell surface.</p>

<p>N-Boc-protected -Guanidino Oseltamivir is a fine chemical that belongs to the group of versatile building blocks. It is a complex compound that has been used in research as a reagent and speciality chemical. N-Boc-protected -Guanidino Oseltamivir is an important intermediate for the synthesis of a variety of useful compounds, such as pharmaceuticals and natural products. This compound is also used as a reaction component in organic syntheses, especially for the preparation of high quality and useful scaffolds.</p>

<p>Cefazaflur is a semisynthetic cephalosporin antibiotic, which is derived from the mold Acremonium (formerly known as Cephalosporium). Its mode of action involves inhibiting bacterial cell wall synthesis by targeting penicillin-binding proteins (PBPs). This interference prevents the cross-linking of peptidoglycan chains, which is essential for bacterial cell wall structural integrity, ultimately leading to cell lysis and death.</p>

<p>Raltegravir is an antiretroviral agent that is used for the treatment of HIV infections. It inhibits HIV integrase in order to prevent viral genome from being inserted into the human genome. It binds to the active site of the enzyme and prevents it from binding to a target sequence on the viral DNA. This drug is metabolized by glucuronidation.</p>

<p>Triclabendazole is a benzimidazole anthelmintic with action on liver flukes by disrupting their microtubule formation and is used for treating fascioliasis in humans and animals.</p>

<p>Inhibitor of protein synthesis; streptogramin</p>

<p>Enoxacin is a fluoroquinolone antibiotic with action on bacterial DNA gyrase and topoisomerase IV and is used for treating urinary tract infections and gonorrhea.</p>

<p>Oritavancin diphosphate is a lipoglycopeptide antibiotic with action on bacterial cell wall synthesis and is used for treating acute bacterial skin and skin structure infections.</p>

<p>Doramectin is a macrocyclic lactone antiparasitic agent with action on glutamate-gated chloride channels in parasites and is used for treating internal and external parasitic infections in livestock.</p>

<p>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.</p>

<p>Dihydrostreptomycin B is an aminoglycoside antibiotic, which is derived from the bacterium Streptomyces griseus. This antibiotic operates by binding to the 30S subunit of the bacterial ribosome, leading to the inhibition of protein synthesis. The binding disrupts the decoding site, causing misreading of mRNA and ultimately resulting in bactericidal activity.</p>

<p>Closantel sodium dihydrate is a salicylanilide antiparasitic agent with action on flukes, nematodes, and arthropods and is used for veterinary treatment of parasitic infections.</p>

<p>Butoconazole nitrate is an antifungal agent and is used for the treatment of vaginal yeast infections. It inhibits the synthesis of ergosterol, disrupting the fungal cell membrane.</p>

<p>Exalamide is an arenecarboxamide antifungal agent with action on fungal growth inhibition and is used for research on fungal infections.</p>

<p>Avermectin B1a (&gt;85%) is a macrolide anthelmintic and is used for the treatment of parasitic infections. It enhances the effects of glutamate at the glutamate-gated chloride channels, causing paralysis and death of the parasite</p>

<p>Gentamicin C1a is an aminoglycoside antibiotic, which is a secondary metabolite derived from the bacterium Micromonospora. This antibiotic functions through a mode of action that involves binding to the 30S subunit of bacterial ribosomes. This binding disrupts protein synthesis by causing misreading of the mRNA, ultimately leading to inhibition of bacterial growth and cellular death.</p>

<p>Erythromycinacistrate is a macrolide antibiotic, which is derived from the bacterium *Saccharopolyspora erythraea*. Its mode of action involves binding to the 50S ribosomal subunit of susceptible bacteria, thereby inhibiting protein synthesis. This action effectively halts bacterial growth and replication, making it particularly effective against a wide range of Gram-positive and some Gram-negative bacteria.</p>

<p>Geneticin is very efficient against gram-negative bacteria, however it is not applied for treating infections due to high renal toxicity. Geneticin and its resistance genes found application in the selection of transgenic cell lines including yeasts such as P. pastoris and S. serevisiae, other eukaryotic cell lines such as CHO or HEK293, but also plant cells and bacterial cells.</p>