Antimicrobials

<p>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.</p>

<p>Chloramphenicol is produced by Streptomyces venezuelae. It is a broad-spectrum antibiotic with bacteriostatic properties. It interferes with bacterial protein synthesis by reversibly binding to the 50S ribosome unit. Used as substrate in the CAT (chloramphenicol acetyl transferase) assay, where the CAT gene expression is monitored by the ability of a system to transform chloramphenicol into acetyl chloramphenicol, which can be followed by simple thin layer chromatography. It is employed in VTM to prevent bacterial growth during specimen storage and transportation.</p>

<p>D-Cycloserine is a antibiotic and NMDA receptor partial agonist with action on bacterial cell wall synthesis and modulation of NMDA receptors and is used for treating tuberculosis and studying neuropsychiatric disorders.</p>

<p>Ceftizoxime sodium is a sodium salt form of ceftizoxime with similar action and applications as ceftizoxime.</p>

<p>Hygromycin B binds near the A site of 16S rRNA and induces errors in the code by inhibition of translocation of peptydil-tRNA, however to a lesser extent compared to other aminoglycosides. Hygromycin B is efficient against bacteria, fungi and other eukaryotic cells, but more often used for the selection of eukaryotic cells including yeasts, such as, P. pastoris and S. cerevisiae, and mammalian cell lines, such as, CHO.</p>

<p>Albomitomycin A is an antibiotic compound, which is derived from the fermentation of specific Streptomyces species. This compound exhibits a unique mode of action by inhibiting protein synthesis in bacterial cells, specifically targeting the 30S ribosomal subunit. This interference with ribosomal function ultimately disrupts the production of essential proteins, leading to bacterial cell death.</p>

<p>Cephalosporin antibiotic; interferes with cell wall biosynthesis</p>

<p>Primaquine is an antimalarial agent with action on Plasmodium hypnozoites in the liver and is used for preventing relapses of malaria caused by Plasmodium vivax and Plasmodium ovale.</p>

<p>Difloxacin HCl is a fluoroquinolone antibiotic with action on bacterial DNA gyrase inhibition and is used for treating bacterial infections in veterinary medicine.</p>

<p>Inhibitor of HCV NS5A</p>

<p>Oxibendazole is a benzimidazole anthelmintic with action on microtubule formation in parasitic worms and is used for treating roundworms, strongyles, and pinworms in horses and pets.</p>

<p>Antiviral; nonpeptidic HIV-1 protease inhibitor</p>

<p>Fosfomycin-beta-D-galactopyranoside sodium is a masked antibiotic which is specifically activated by the enzyme beta-galactosidase. The compound can be cleaved by organsims expressing beta-galactosidase, leading to release of unmasked fosfomycin and thus auto-inhibition. Fosfomycin is a broad-spectrum cell wall active agent that inhibits the MurA enzyme involved in peptidoglycan synthesis of bacteria.</p>

<p>Cefaloram is a cephalosporin antibiotic with action on bacterial cell wall synthesis and is used for treating bacterial infections.</p>

<p>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.</p>

<p>Chemically derived from ritonavir, Lopinavir belongs to the amphetamines. Lopinavir is clinically used in the prevention and treatment of HIV infections as it acts as HIV-1 protease inhibitor. In 2020, lopinavir was tested to treat COVID-19 patients and although it led to a higher rate of gastrointestinal side effects, the Lopinavir-treated group had a lower incidence of severe complications. Overall it was deemed not to work as a treatment.</p>

<p>Chemotherapy for bladder cancer; semi-synthetic analog of doxorubicin</p>

<p>Cinoxacin is a quinolone antibiotic with action on bacterial DNA synthesis inhibition and is used for treating urinary tract infections.</p>

<p>Bacteriostatic; for treating multi-drug-resistant tuberculosis</p>

<p>Naturally produced by the soil bacterium Streptomyces avermitili, Ivermectin is clinically used in the treatment of parasitosis in both humans and animals. Ivermectin is commercially available as a mixture of 80% 22, 23-dihydroavermectin B1a and 20% 22, 23-dihydroavermectin B1b. In 2020, research indicated that it was a good antiviral agent in the treatment of SARS-CoV-2 and a new mechanism of action has been suggested. Ivermectin would act on importin α/β heterodimer and affect nuclear transport and the translocation of viral proteins.</p>

<p>STAADIUM™ GlucuroniZide is a targeted inhibitor of glucuronidase-producing bacteria, which is activated by E. coli-specific glucuronidase enzyme. Glucuronidases are enzymes catalysing the cleavage of complex carbohydrates and E. coli is a well-known producer. In complex cultures, E. coli strains often outcompete bacteria that present at lower titre and STAADIUM™ GlucuroniZide can help to selectively reduce the growth of E. coli. STAADIUM™ GlucuroniZide can be used in microbiome studies, food control, environmental safety, hygiene, and clinical diagnostics. More details can be found in the application notes document.</p>

<p>A competitive inhibitor of HCV NS3/4A protease that blocks viral replication. Efficacious in treating HCV-infected patients in combination with daclatasvir. Asunaprevir-resistant replicons are sensitive to NS5A replication complex inhibitor, suggesting potential combination therapy.</p>

<p>(S)-6,7-Dihydro-2-nitro-6-[[4-(trifluoromethoxy)phenyl]methoxy]-5H-imidazo[2,1-b][1,3]oxazine ia slo known as PA-824. An anti-tuberculosis drug that affects both replicating and non-replicating Mycobacterium tuberculosis via cell wall inhibition and respiratory poisoning..</p>

<p>Antibiotic; anti-protozoal; anti-helmintic; protein synthesis inhibitor</p>

<p>α-Apo-oxytetracycline is a degradation product of oxytetracycline with action on bacterial protein synthesis inhibition and is used for research on antibiotic activity and bacterial resistance.</p>

<p>Gatifloxacin is an antibiotic, which is a synthetic fluoroquinolone with broad-spectrum antibacterial activity. Its source lies in its chemical synthesis, designed to inhibit bacterial enzymes necessary for DNA replication. The mode of action involves the inhibition of bacterial DNA gyrase and topoisomerase IV, which are critical enzymes for bacterial DNA replication, transcription, and repair. This dual inhibitory mechanism disrupts bacterial cell division and growth, leading to the eventual eradication of susceptible bacterial strains.</p>

<p>Meropenem trihydrate has broad spectrum activity against Gram-positive and Gram-negative bacteria, as well as, some mycoplasma species. It inhibits cell wall synthesis by binding to bacterial penicillin-binding proteins (PBP), which impairs cell wall integrity, induces the formation of reactive oxygen species, and inhibits macromolecular synthesis in bacteria. It can be used to prevent bacterial growth after being exposed to meropenem through fluorescence imaging of human blood plasma. Meropenem trihydrate research studies showed a reduction of the allergen levels in patients with respiratory allergies or asthma, specifically dust mites, cockroaches, animal dander, pollen grains, etc. by inhibit allergen-induced sensitization of mast cells.</p>

<p>Cephalothin sodium is a first-generation cephalosporin antibiotic with action on bacterial cell wall synthesis and is used for treating bacterial infections such as respiratory tract infections and skin infections.</p>

<p>Benethamine penicillin is a beta-lactam antibiotic, which is a semi-synthetic derivative of penicillin. It is sourced from the modification of naturally occurring penicillin compounds, typically produced through the fermentation of Penicillium mold cultures. Benethamine penicillin operates by inhibiting bacterial cell wall synthesis. It targets the penicillin-binding proteins within bacterial cell membranes, disrupting peptidoglycan cross-linking, which is essential for cell wall structural integrity. This leads to cell lysis and death in susceptible bacteria.</p>

<p>Orbifloxacin is a fluoroquinolone antibiotic with action on bacterial DNA gyrase and topoisomerase IV and is used for treating bacterial infections in veterinary medicine.</p>

<p>Versalide is a synthetic musk compound with action as a fragrance ingredient and is used for adding scent to perfumes and personal care products.</p>

<p>Herbicidin K is a naturally derived herbicide, known for its biological origin from microbial fermentation processes. It is primarily sourced from certain strains of Streptomyces, a genus of Gram-positive bacteria notable for their diverse secondary metabolites. The mode of action of Herbicidin K involves the inhibition of key enzymatic pathways within target plants, leading to the disruption of cellular functions and ultimately plant death. This selectivity is particularly effective against broadleaf weeds, providing a targeted approach to weed management.</p>

<p>Griselimycin is an antibiotic, which is derived from the bacterial genus *Streptomyces*. This compound exhibits its mode of action by targeting bacterial protein synthesis, specifically binding to the DNA polymerase sliding clamp, thereby inhibiting replication and cell division in a range of bacterial pathogens. Griselimycin has been the focus of renewed scientific interest due to its potent activity against Mycobacterium tuberculosis, including multi-drug-resistant strains. The compound’s unique mode of action makes it a promising candidate for further development in the treatment of tuberculosis and potentially other bacterial infections that have developed resistance to more commonly used antibiotics. Advances in understanding its biosynthesis have facilitated semi-synthetic modifications, potentially enhancing its pharmacokinetic properties and antimicrobial spectrum. The applications of Griselimycin extend to research contexts where understanding resistance mechanisms and novel antibiotic development are critical. Continued exploration of this compound may contribute significantly to addressing the global challenge of antibiotic resistance.</p>

<p>HIV-1 Integrase Inhibitor is an antiretroviral compound with a mode of action that blocks the viral enzyme integrase, preventing the integration of viral DNA into the host genome. It is used for the treatment of HIV infection.</p>

<p>2-Methyl-4-isothiazolin-3-one or MIT is a powerful antimicrobial and antifungal agent which is widely used in personal care products. It is also used in industrial applications as a preservative and antifouling agent.</p>

<p>Fementation intermediate of Oritavancin</p>

<p>Cefacetrile is a first-generation cephalosporin antibiotic with action on bacterial cell wall synthesis and is used for treating bacterial infections in humans and animals.</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>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>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>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>Inhibitor of protein synthesis; aminoglycoside</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>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>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>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>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>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>Inhibits DNA gyrase and topoisomerase IV</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>Norfloxacin 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>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>Broad-spectrum antibiotic; bacterial cell wall biogenesis inhibitor</p>

<p>Epioxytetracycline is a degradation product of the antibiotic oxytetracycline. It has been found in wastewater.</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>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>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>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>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>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>Inhibitor of protein synthesis; steroid antibiotic</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>Enrofloxacin is a rapidly bactericidal antibiotic, that inhibits bacterial growth by binding to the 50S ribosomal subunit and blocking protein synthesis, thereby preventing the bacteria from making new proteins. Enrofloxacin also has strong activity against gram-positive bacteria, including Clostridium perfringens which is an anaerobic bacterium that causes food-borne illness. This antibiotic is used for the treatment of acute bacterial infections in humans, such as, skin or soft tissue infections, urinary tract infections (UTIs) and septicemia (bloodstream infection). Enrofloxacin has shown excellent bioavailability with high serum protein binding capacity. Additionally, it has good efficacy against clinical isolates of Escherichia coli and Klebsiella pneumoniae. Enrofloxacin can be used effective in treatments for Pseudomonas aeruginosa and Enterobacter species.</p>

<p>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.</p>

<p>Tenofovir diphosphate triethylamine (mixture of diastereomers) is an antiviral compound, which is a synthetic chemical product derived from the parent compound, tenofovir. This formulation includes a mixture of diastereomers to enhance its solubility and bioavailability. The compound primarily functions as a nucleotide reverse transcriptase inhibitor (NRTI). It targets viral reverse transcriptase enzymes, inhibiting DNA synthesis and subsequent viral replication by causing premature chain termination.</p>

<p>Cefuroxime is a second-generation cephalosporin antibiotic with action on bacterial cell wall synthesis and is used for treating respiratory tract infections, urinary tract infections, and Lyme disease.</p>

<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>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>Antibiotic of fluoroquinolone class; DNA replication inhibitor</p>

<p>Ceftriaxone is a broad-spectrum cephalosporin antibiotic that is used for the treatment of bacterial infections in different locations such as the skin, soft tissue and respiratory tract. This drug works by inhibiting mucopeptide synthesis in the bacterial cell wall. As a result, bacteria will produce defective cell walls leading to cell death.</p>

<p>Pirazinecarboxamide (Pyrazinamide) is an antitubercular agent with action on Mycobacterium tuberculosis by disrupting membrane energetics and is used for treating tuberculosis in combination with other drugs.</p>

<p>Cefadroxil monohydrate is a hydrated form of cefadroxil with similar action and applications as cefadroxil.</p>

<p>Nucleoside analog with antiviral activity against zoonotic feline infectious peritonitis virus (FIPV) and severe acute respiratory syndrome (SARS) virus from Coronaviridae family. The compound is a pro-drug and undergoes intracellular phosphorylation resulting in the active triphosphate metabolite. The triphosphorylated GS 441524 analog competes with natural nucleoside triphosphates and interferes with viral RNA synthesis. In previous studies it was tested in vitro as well as in experimental animals and showed good safety profile.</p>

<p>Darunavir is a HIV-1 protease inhibitor used orally in the treatment of patients with multi-drug resistant HIV-1 infection (Ghosh, 2007). It has also been shown to be effective against other infectious diseases such as hepatitis C virus and SARS coronavirus. Metabolized by cytochrome P450 3A (CYP3A) isoenzymes, darunavir is often administered together with ritonavir that prolongs its bioavaiability, giving a terminal elimination half-life (t1/2) of 15 hours (Back, 2008). The effect of darunavir on natural compounds such as matrix proteins and toll-like receptor activity has also been studied via high performance liquid chromatography (HPLC) experiments.</p>

<p>Cefozopran hydrochloride is a fourth-generation cephalosporin antibiotic with action on bacterial cell wall synthesis and is used for treating severe bacterial infections, including those caused by resistant strains.</p>

<p>Dibekacin sulfate is an aminoglycoside antibiotic with action on bacterial protein synthesis inhibition and is used for treating severe gram-negative bacterial infections.</p>

<p>Anthracycline is a class of chemotherapy drugs, which are anthraquinone antibiotics derived from the bacterial genus Streptomyces. They exert their therapeutic effects primarily through intercalation into DNA, disrupting the function of enzymes such as topoisomerase II, thus preventing the transcription and replication processes in rapidly dividing cancer cells. Furthermore, they generate free radicals, leading to oxidative stress and subsequent cell damage. These mechanisms collectively result in apoptosis of malignant cells. Anthracyclines are utilized extensively in oncology for the treatment of various malignancies, including leukemias, lymphomas, breast cancer, and sarcomas. The efficacy of anthracyclines in inhibiting tumor growth must be balanced against their cardiotoxic potential, which is a significant consideration in their clinical use. This dual nature makes them both pivotal and challenging in chemotherapy regimens, necessitating careful management and monitoring throughout treatment.</p>

<p>Abacavir is an antiviral nucleoside reverse transcriptase inhibitor that is used for the treatment of HIV. This drug inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with dGTP and by its incorporation into viral DNA.</p>

<p>Faropenem sodium hemipentahydrate is a penem-class beta-lactam antibiotic with action on bacterial cell wall synthesis and is used for treating respiratory, skin, and urinary tract infections.</p>

<p>Tiamulin fumarate is a pleuromutilin antibiotic with action on bacterial protein synthesis by targeting the 50S ribosomal subunit and is used for treating swine dysentery and respiratory infections in livestock.</p>