Antimicrobianos

<p>Neospiramycin I is a macrolide antibiotic with action on bacterial ribosomes to inhibit protein synthesis and is used for treating bacterial infections in research applications.</p>

<p>Atovaquone is an antimicrobial drug that is used for the treatment of Pneumocystis jirovecii pneumonia. This drug is an analog of ubiquinone and has good in vitro activity against Toxoplasma gondii.</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>b-Apo-oxytetracycline is a tetracycline antibiotic and is used for the treatment of bacterial infections. It binds to the 30S ribosomal subunit, inhibiting protein synthesis.</p>

<p>Boromycin is a macrolide antibiotic, which is derived from the fermentation of certain strains of Streptomyces bacteria. It operates as an ionophore with the ability to transport ions across lipid membranes, effectively disrupting ionic gradients. This mechanism of action compromises essential cellular processes in target organisms, thereby exerting its antimicrobial effects.</p>

<p>Fostriecin is a potent anticancer agent, which is a natural product isolated from the bacterium Streptomyces pulveraceus. It acts primarily as an inhibitor of protein phosphatases, particularly protein phosphatase 2A (PP2A) and protein phosphatase 4 (PP4), functioning by blocking their catalytic activity. This inhibition disrupts cell cycle regulation, leading to apoptosis in cancer cells.</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>A broad-spectrum antibiotic of cephalosporin class, which inhibits bacterial cell wall synthesis by targeting the penicillin-binding protein, involved in peptidoglycan synthesis. This third-generation cephalosporin is very active against Pseudomonas species and can also be used to treat bacterial meningitis as it penetrates in the cerebrospinal fluid.</p>

<p>Bedaquiline fumarate is the salt form of bedaquiline, a diarylquinoline molecule with an ATP synthetase inhibitory activity. Bedaquiline fumarate is an FDA-approved drug for the oral treatment of multidrug-resistant tuberculosis. Bedaquiline fumarate acts by inhibiting the activity of the ATP synthetase in the pathogenic bacterium Mycobacterium tuberculosis, even in the case of multiple antibiotic resistant strains.</p>

<p>Lamivudine (commonly called 3TC) is a potent nucleoside analogue reverse transcriptase inhibitor. It is one of the front line treatments for HIV.  It is an analogue of cytidine, and can inhibit both types (1 and 2) of HIV reverse transcriptase as well as the reverse transcriptase of hepatitis B. It needs to be phosphorylated to its triphosphate form before it is active.</p>

<p>Inhibitor of isoleucyl-tRNA synthetase; inhibitor of protein synthesis</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>Netilmicin sulfate is an aminoglycoside antibiotic with action on bacterial protein synthesis by binding to the 30S ribosomal subunit and is used for treating severe bacterial infections.</p>

<p>Tilmicosin is a macrolide antibiotic that is used in veterinary medicine. It is used to treat bovine respiratory disease and inhibits bacterial growth by binding to the 50S ribosomal subunit of the bacteria resulting in reduced protein synthesis.</p>

<p>Antibiotic of fluoroquinolone class; DNA replication inhibitor</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>Saquinavir is a HIV protease inhibitor drug that is used with other antiretroviral drugs for the treatment of HIV-1. As this drug prevents HIV protease activity, it prevents the proteolysis of the Gag polyprotein and thus results in non-infectious virus particles.</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>Sitafloxacin sesquihydrate is a fourth-generation fluoroquinolone antibiotic with action on bacterial DNA gyrase and topoisomerase IV and is used for treating respiratory, urinary, and gastrointestinal infections.</p>

<p>Anti-viral; non-nucleoside reverse transcriptase inhibitor</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>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>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>Nitrocycline is a broad-spectrum antibiotic, which is a synthetic derivative of tetracycline with enhanced antibacterial properties. As a chemically synthesized compound, nitrocycline has been engineered to overcome resistance mechanisms common in bacterial pathogens. Its mode of action involves the inhibition of protein synthesis, achieved by binding to the 30S ribosomal subunit, effectively preventing the addition of new amino acids to nascent peptide chains. This binding action interrupts bacterial growth and replication, providing robust activity against both Gram-positive and Gram-negative bacteria.</p>

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

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

<p>Tylosin tartrate is a macrolide antibiotic with action on bacterial protein synthesis inhibition and is used for treating bacterial infections in livestock and poultry.</p>

<p>Cefuroxime axetil is a prodrug of cefuroxime with action on bacterial cell wall synthesis and is used for treating bacterial infections like sinusitis, bronchitis, and gonorrhea.</p>

<p>Clofazimine is a phenazine dye antibiotic with action on bacterial DNA interference and is used for treating leprosy and erythema nodosum leprosum.</p>

<p>25-Desacetylrifampin is the main metabolite of rifampicin, used in the treatment of tuberculosis. 25-Desacetylrifampin has partial actvity.</p>

<p>Cidofovir is an anti-viral agent that is used to treat Cytomegalovirus (CMV) retinitis in patients with AIDS. This drug suppresses CMV replication by inhibiting viral DNA synthesis.</p>

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

<p>Piperacillin sodium, pharma grade is a pharmaceutical-grade beta-lactam antibiotic with action on bacterial cell wall synthesis and is used for research and pharmaceutical applications.</p>

<p>Membrane-disrupting agent; cationic peptide</p>

<p>6-Fluoro-3-hydroxypyrazine-2-carboxamide is a potent RNA polymerase inhibitor, active against both RNA viruses in vitro and in vivo. A four-step approach to the synthesis of 6-Fluoro-3-hydroxypyrazine-2-carboxamide was reported in 2014. 6-Fluoro-3-hydroxypyrazine-2-carboxamide is commercialized and has recently been suggested for the treatment of mild cases of COVID-19.</p>

<p>Amrubicin hydrochloride is an anthracycline chemotherapeutic agent, which is a synthetic anthracycline derivative derived from reductive amination. It functions primarily by intercalating into DNA and inhibiting topoisomerase II, an enzyme crucial to DNA replication. This mode of action disrupts DNA synthesis, leading to apoptosis in rapidly proliferating cancer cells.</p>

<p>Fenbendazole is a benzimidazole anthelmintic with action on microtubule formation in parasites and is used for treating gastrointestinal parasites in animals.</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>Antibacterial used in treatment of UTI and respiratory tract infections</p>

<p>Fosamprenavir calcium is an antiretroviral medication, which is derived from the prodrug of amprenavir. It is synthesized through chemical processes to enhance oral bioavailability and improve pharmacokinetic properties. Through its mode of action, fosamprenavir is converted in vivo to amprenavir, which acts as an inhibitor of the HIV-1 protease enzyme. By inhibiting this enzyme, it prevents the cleavage of the Gag-Pol polyprotein, disrupting viral replication and processing, ultimately leading to the production of immature, non-infectious viral particles.</p>

<p>Nifursol is a nitrofuran veterinary antibiotic with action on protozoal growth inhibition and is used for preventing histomoniasis in poultry.</p>

<p>Dirithromycin is a macrolide glycopeptide antibiotic with action on bacterial protein synthesis inhibition and is used for treating respiratory, skin, and other bacterial infections.</p>

<p>Piperaquine tetraphosphate tetrahydrate is an antimalarial compound with action on Plasmodium parasites by disrupting DNA synthesis and is used for treating malaria in combination therapies.</p>

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

<p>Fenticonazole nitrate is an imidazole antifungal agent with action on fungal cell membrane disruption and is used for treating fungal infections like vaginal thrush and athlete's foot.</p>

<p>Isomitomycin A is a naturally occurring microbial metabolite, which is isolated from certain strains of actinomycetes. It exhibits a unique mode of action by interfering with viral replication processes, effectively inhibiting the proliferation of various viral pathogens. The alkaloidal structure of Isomitomycin A allows it to integrate into nucleic acid processing pathways, eventually disrupting the function and synthesis of viral genomes.</p>

<p>Alloaureothin is an antibacterial compound, which is a secondary metabolite derived from the bacterial genus *Streptomyces*. This compound functions through a distinct mode of action, primarily targeting bacterial cell components and inhibiting essential growth processes. Alloaureothin disrupts cell wall synthesis and cellular metabolism, leading to effective bacteriostatic or bactericidal outcomes depending on the concentration and specific bacterial species.</p>

<p>Lucimycin is an antibiotic, which is derived from the fermentation of specific Streptomyces bacterial strains. This compound exerts its antibacterial effects by binding to the 50S subunit of the bacterial ribosome, thereby inhibiting protein synthesis and effectively halting bacterial growth. Lucimycin is particularly effective against Gram-positive bacteria and some Gram-negative species, making it a valuable tool in both clinical and research settings.</p>

<p>A sulfanilide anti-bacterial agent used to treat various skin diseases</p>

<p>Amdinocillin is a semisynthetic antibiotic with broad-spectrum activity that is part of the aminopenicillin family. It is used in the treatment of bacterial infections such as those caused by Gram-negative bacteria, and to treat methicillin-resistant Staphylococcus (MRSA). The clinical isolate Amdinocillin has an inhibitory concentration (IC) of 0.25 μg/mL against Enterobacter aerogenes and Enterobacter cloacae, and it displays a synergistic effect in combination with other antibiotics. The mechanism of action is that prevents bacterial growth and proliferation by inhibiting cell wall synthesis and causing lysis, which allows for drug therapy against specific types of bacteria.</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>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>Itraconazole is an anti-fungal drug that inhibits the synthesis of ergosterol, a component of the fungal cell membrane. Itraconazole is in a class of antifungals called triazoles. The drug binds to ergosterol in the fungal cell membrane and prevents it from being inserted into the membrane. This decreases the permeability of the plasma membrane, causing leakage of cellular contents. Additionally, it has been shown to have a glucose-lowering effect in the treatment of acute leukaemia and may be used for research in aiding to diagnose hematopoietic stem cell or leukaemia.</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>Potent inhibitor of viral RNA polymerase called non-structural protein 5B (NS5B). This nucleotide analog is effective against Hepatitis C virus (HCV) infection since it inhibits viral RNA replication. Sofosbuvir is a prodrug and gets triphosphorylated in the liver cells, generating biologically active compound with anti-viral activity.</p>

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

<p>Nalidixic acid is a quinolone antibiotic with action on bacterial DNA gyrase to inhibit DNA replication and is used for treating urinary tract infections caused by gram-negative bacteria.</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>Triazavirin is an antiviral drug developed against SAR-CoV-2. The action of triazavirin might be due to its ability to inhibit the Mpro protease from SARS viruses. Triazavirin has been clinically tested in the treatment of COVID-19 patients.</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>Cefiderocol is a siderophore cephalosporin antibiotic with action on bacterial cell wall synthesis, particularly targeting multidrug-resistant gram-negative bacteria and is used for treating complicated urinary tract infections and hospital-acquired pneumonia.</p>

<p>Tetracycline hydrochloride - USP is a broad-spectrum antibiotic, which is a synthetic derivative of chlortetracycline produced from the bacterium *Streptomyces aureofaciens*. It functions by inhibiting protein synthesis in bacteria, specifically binding to the 30S ribosomal subunit. This action prevents the attachment of aminoacyl-tRNA to the mRNA-ribosome complex, thereby halting bacterial growth and replication.</p>

<p>Dequalinium chloride is a quaternary ammonium compound that has been discovered to be an inhibitor of the cytopathic effects of some syndrome viruses. It is able to inhibit the replication of the virus in various clinical isolates and in cell culture models. Dequalinium chloride also inhibits acetylcholine receptor-mediated endocytosis, which is one of the mechanisms by which cells resist infection. The mechanism by which dequalinium chloride inhibits acetylcholine receptor-mediated endocytosis is not yet known, but it has been suggested that it might be due to its inhibitory activity on mitochondrial uncoupler proteins. This property may make dequalinium chloride an effective treatment against bacterial infections and respiratory diseases such as cystic fibrosis and asthma.</p>

<p>Teicoplanin is related to vancomycin and has similar effects against gram-positive bacteria and anaerobes, and usually requires less frequent administration than vancomycin, but it is less efficient against S. haemolyticus. Due its size and polarity, teicoplanin can’t pass through the membrane of gram-negative bacteria thus it is not active against them. It is used to treat severe infections such as septicemia, endocarditis, bone and joint infections.</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>Apramycin sulfate is a semisynthetic antibiotic that inhibits the growth of Gram-negative bacteria. It is a sulfonamide and has been used in clinical isolates to treat bacterial infections. Apramycin sulfate inhibits the biosynthesis of folic acid, which is important for DNA synthesis and cell division. It also inhibits the production of RNA by binding to ribosomes and inhibiting protein synthesis. Apramycin has been shown to have anticancer properties as well, with studies showing that it can inhibit tumor growth in vitro and in vivo.</p>

<p>Antibiotic of penicillin class; inhibits bacterial cell wall biogenesis</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>Levofloxacin Hemihydrate is a fluoroquinolone antibiotic with a mode of action that inhibits bacterial DNA gyrase and topoisomerase IV. It is used for treating bacterial infections, similar to its anhydrous form.</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>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>STAADIUMTM PhosphoZide is a targeted inhibitor of phosphatase-producing bacteria, which is activated by phosphatase itself. STAADIUMTM 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. STAADIUMTM 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>Antibiotic of tetracycline class; protein synthesis inhibitor</p>

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

<p>Cefuroxime sodium is a sodium salt form of cefuroxime with similar action and applications as cefuroxime.</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>Broad-spectrum antibiotic; bacterial cell wall biogenesis inhibitor</p>

<p>Ombitasvir is a NS5A inhibitor antiviral agent with action on hepatitis C virus replication and is used for treating chronic hepatitis C in combination therapies.</p>

<p>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.</p>

<p>Herbicidin C is an antibiotic, which is derived from a microbial source, specifically from certain strains of actinobacteria. This compound functions as an inhibitor, interfering with specific metabolic pathways within target organisms. Its mode of action involves disrupting the synthesis of critical proteins, which are essential for cell survival and growth.</p>

<p>β-lactam antibiotic of penicillin subclass, which inhibits bacterial cell wall synthesis by targeting the proteoglycan synthesis. Cloxacillin has a narrow spectrum of action and is effective against Gram-positive organisms. Cloxacillin is resistant to the action of β-lactamase and therefore preferentially used for treatment of Staphylococcal infections.</p>

<p>Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) medication used in the treatment of human immunodeficiency virus (HIV) infections. It works by blocking reverse transcriptase, an enzyme essential for replication of the virus, thereby preventing the virus from multiplying and spreading. Etravirine is often used in combination with other antiretroviral drugs to effectively treat HIV/AIDS. It is commonly prescribed for patients with virus strains that are resistant to other NNRTI medications due to mutations that confer resistance- mutations K103N and Y181C. Etravirine is a diarylpyrimidine (DAPY) and has conformational isomerism meaning that it binds reverse transcriptase in an fleible manner, under multiple conformations. The impact of specific point mutations in the virus is therefore lessened.</p>