Eravacycline Structure
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Eravacycline Structure
Eravacycline (TP-434, Xerava) is a synthetic halogenated tetracycline class antibiotic by Tetraphase Pharmaceuticals. It is closely related to tigecycline. It has a broad spectrum of activity including many multi-drug resistant strains of bacteria. Phase III studies in complicated intra-abdominal infections (cIAI) and complicated urinary tract infections (cUTI) were recently completed with mixed results. Eravacycline was granted fast track designation by the FDA and is currently available in USA. Medical uses Eravacycline has shown broad spectrum of activity against a variety of Gram-positive and Gram-negative bacteria, including multi-drug resistant strains, such as methicillin-resistant ''Staphylococcus aureus'' (MRSA) and carbapenem-resistant Enterobacteriaceae. It is currently being formulated as for intravenous and oral administration. Spectrum of activity Gram-positive organisms * ''Staphylococcus aureus'' (both methicillin-resistant and sensitive strains) * ''Str ...
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Halogenated
In chemistry, halogenation is a chemical reaction that entails the introduction of one or more halogens into a compound. Halide-containing compounds are pervasive, making this type of transformation important, e.g. in the production of polymers, drugs. This kind of conversion is in fact so common that a comprehensive overview is challenging. This article mainly deals with halogenation using elemental halogens (F2, Cl2, Br2, I2). Halides are also commonly introduced using salts of the halides and halogen acids. Many specialized reagents exist for and introducing halogens into diverse substrates, e.g. thionyl chloride. Organic chemistry Several pathways exist for the halogenation of organic compounds, including free radical halogenation, ketone halogenation, electrophilic halogenation, and halogen addition reaction. The nature of the substrate determines the pathway. The facility of halogenation is influenced by the halogen. Fluorine and chlorine are more electrophilic and ...
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Moraxella Catarrhalis
''Moraxella catarrhalis'' is a fastidious, nonmotile, Gram-negative, aerobic, oxidase-positive diplococcus that can cause infections of the respiratory system, middle ear, eye, central nervous system, and joints of humans. It causes the infection of the host cell by sticking to the host cell using trimeric autotransporter adhesins. Epidemiology ''Moraxella catarrhalis'' is a human pathogen with an affinity for the human upper respiratory tract. Other primates, such as macaques, might become infected by this bacterium. History ''Moraxella catarrhalis'' was previously placed in a separate genus named ''Branhamella''. The rationale for this was that other members of the genus ''Moraxella'' are rod-shaped and rarely caused infections in humans. However, results from DNA hybridization studies and 16S rRNA sequence comparisons were used to justify inclusion of the species ''M. catarrhalis'' in the genus ''Moraxella''. As a consequence, the name ''Moraxella catarrhalis'' is cur ...
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Meropenem
Meropenem, sold under the brand name Merrem among others, is an intravenous β-lactam antibiotic used to treat a variety of bacterial infections. Some of these include meningitis, intra-abdominal infection, pneumonia, sepsis, and anthrax. Common side effects include nausea, diarrhea, constipation, headache, rash, and pain at the site of injection. Serious side effects include ''Clostridioides difficile'' infection, seizures, and allergic reactions including anaphylaxis. Those who are allergic to other β-lactam antibiotics are more likely to be allergic to meropenem as well. Use in pregnancy appears to be safe. It is in the carbapenem family of medications. Meropenem usually results in bacterial death through blocking their ability to make a cell wall. It is more resistant to breakdown by β-lactamase producing bacteria. Meropenem was patented in 1983. It was approved for medical use in the United States in 1996. It is on the World Health Organization's List of Essential Med ...
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Colistin
Colistin, also known as polymyxin E, is an antibiotic medication used as a last-resort treatment for multidrug-resistant Gram-negative infections including pneumonia. These may involve bacteria such as ''Pseudomonas aeruginosa'', ''Klebsiella pneumoniae'', or ''Acinetobacter''. It comes in two forms: colistimethate sodium can be injected into a vein, injected into a muscle, or inhaled, and colistin sulfate is mainly applied to the skin or taken by mouth. Colistimethate sodium is a prodrug; it is produced by the reaction of colistin with formaldehyde and sodium bisulfite, which leads to the addition of a sulfomethyl group to the primary amines of colistin. Colistimethate sodium is less toxic than colistin when administered parenterally. In aqueous solutions it undergoes hydrolysis to form a complex mixture of partially sulfomethylated derivatives, as well as colistin. Resistance to colistin began to appear as of 2015. Common side effects of the injectable form include kidn ...
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Polymyxin B
Polymyxin B, sold under the brand name Poly-Rx among others, is an antibiotic used to treat meningitis, pneumonia, sepsis, and urinary tract infections. While it is useful for many Gram negative infections, it is not useful for Gram positive infections. It can be given by injection into a vein, muscle, or cerebrospinal fluid or inhaled. The injectable form is generally only used if other options are not available. It is also available as the combinations bacitracin/polymyxin B and neomycin/polymyxin B/bacitracin for use on the skin. Common side effects when given by injection include kidney problems, neurological problems, fever, itchiness, and rash. Injections into muscle may result in significant pain. Other serious side effects may include fungal infections, anaphylaxis, and muscle weakness. It is unclear if use during pregnancy is safe for the baby. Polymyxin B works by breaking down the cytoplasmic membrane which generally results in bacterial cell death. Polymyxin B wa ...
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Serratia Marcescens
''Serratia marcescens'' () is a species of rod-shaped, Gram-negative bacteria in the family Yersiniaceae. It is a facultative anaerobe and an opportunistic pathogen in humans. It was discovered in 1819 by Bartolomeo Bizio in Padua, Italy.Serratia marcescens. (2011, April). Retrieved from https://microbewiki.kenyon.edu/index.php/Serratia_marcescens ''S. marcescens'' is commonly involved in hospital-acquired infections (HAIs), also called nosocomial infections, particularly catheter-associated bacteremia, urinary tract infections, and wound infections, and is responsible for 1.4% of HAI cases in the United States. It is commonly found in the respiratory and urinary tracts of hospitalized adults and in the gastrointestinal systems of children. Due to its abundant presence in the environment, and its preference for damp conditions, ''S. marcescens'' is commonly found growing in bathrooms (especially on tile grout, shower corners, toilet water lines, and basins), where it manife ...
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Proteus Mirabilis
''Proteus mirabilis'' is a Gram-negative, facultatively anaerobic, rod-shaped bacterium. It shows swarming motility and urease activity. ''P. mirabilis'' causes 90% of all ''Proteus'' infections in humans. It is widely distributed in soil and water. ''Proteus mirabilis'' can migrate across the surface of solid media or devices using a type of cooperative group motility called swarming. ''Proteus mirabilis'' is most frequently associated with infections of the urinary tract, especially in complicated or catheter-associated urinary tract infections. Diagnosis An alkaline urine sample is a possible sign of ''P. mirabilis''. It can be diagnosed in the lab due to characteristic swarming motility, and inability to metabolize lactose (on a MacConkey agar plate, for example). Also ''P. mirabilis'' produces a very distinct fishy odor. Disease This rod-shaped bacterium has the ability to produce high levels of urease, which hydrolyzes urea to ammonia (NH3), so makes the urine more a ...
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Citrobacter
''Citrobacter'' is a genus of Gram-negative coliform bacteria in the family Enterobacteriaceae. The species ''C. amalonaticus'', ''C. koseri'', and ''C. freundii'' can use citrate as a sole carbon source. ''Citrobacter'' species are differentiated by their ability to convert tryptophan to indole (''C. koseri'' is the only citrobacter to be commonly indole-positive), ferment lactose (''C. koseri'' is a lactose fermentor), and use malonate. ''Citrobacter'' shows the ability to accumulate uranium by building phosphate complexes. Clinical significance These bacteria can be found almost everywhere in soil, water, wastewater, etc. They can also be found in the human intestine. They are rarely the source of illnesses, except for infections of the GI Tract, urinary tract and infant meningitis and sepsis. ''Citrobacter freundii'' strains have inducible ''ampC'' genes encoding resistance to ampicillin and first-generation cephalosporins. In addition, isolates of ''Citrobacter'' may be r ...
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Enterobacter
''Enterobacter'' is a genus of common Gram-negative, facultatively anaerobic, rod-shaped, non-spore-forming bacteria of the family Enterobacteriaceae. It is the type genus of the order Enterobacterales. Several strains of these bacteria are pathogenic and cause opportunistic infections in immunocompromised (usually hospitalized) hosts and in those who are on mechanical ventilation. The urinary and respiratory tracts are the most common sites of infection. The genus ''Enterobacter'' is a member of the coliform group of bacteria. It does not belong to the fecal coliforms (or thermotolerant coliforms) group of bacteria, unlike ''Escherichia coli'', because it is incapable of growth at 44.5 °C in the presence of bile salts. Some of them show quorum sensing properties. One clinically important species from this genus is '' E. cloacae''. Researchers in 2018 reported, after detecting the presence on the International Space Station (ISS) of five '' Enterobacter bugandensis'' b ...
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Klebsiella Oxytoca
''Klebsiella oxytoca'' is a Gram-negative, rod-shaped bacterium that is closely related to ''K. pneumoniae'', from which it is distinguished by being indole-positive; it also has slightly different growth characteristics in that it is able to grow on melezitose, but not 3-hydroxybutyrate. It was first described in 1886 when it was isolated from sour milk and named ''Bacillus oxytocus perniciosus'' (from Greek ''oxus'' 'sour' + ''-tokos'' 'producing'). ''Klebsiella oxytoca'' is characterized by negative methyl red, positive VP, positive citrate, urea and TSI gas production, is AA, and negative for TSI sulfide, DNAse, growth on sulfide-indole motility medium and the phenylalanine deaminase test. It is a diazotroph, able to colonise plant hosts and fix atmospheric nitrogen into a form which the plant can use. Association of ''K. oxytoca'' with the barley rhizosphere during an entire vegetative period has been demonstrated. The bacteria adhere strongly to root hairs, and less stron ...
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Klebsiella Pneumoniae
''Klebsiella pneumoniae'' is a Gram-negative, non-motile, encapsulated, lactose-fermenting, facultative anaerobic, rod-shaped bacterium. It appears as a mucoid lactose fermenter on MacConkey agar. Although found in the normal flora of the mouth, skin, and intestines, it can cause destructive changes to human and animal lungs if aspirated, specifically to the alveoli resulting in bloody, brownish or yellow colored jelly like sputum. In the clinical setting, it is the most significant member of the genus ''Klebsiella'' of the Enterobacteriaceae. ''K. oxytoca'' and ''K. rhinoscleromatis'' have also been demonstrated in human clinical specimens. In recent years, ''Klebsiella'' species have become important pathogens in nosocomial infections. It naturally occurs in the soil, and about 30% of strains can fix nitrogen in anaerobic conditions. As a free-living diazotroph, its nitrogen-fixation system has been much-studied, and is of agricultural interest, as ''K. pneumoniae'' has been ...
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Beta-lactamase
Beta-lactamases, (β-lactamases) are enzymes () produced by bacteria that provide multi-resistance to beta-lactam antibiotics such as penicillins, cephalosporins, cephamycins, monobactams and carbapenems (ertapenem), although carbapenems are relatively resistant to beta-lactamase. Beta-lactamase provides antibiotic resistance by breaking the antibiotics' structure. These antibiotics all have a common element in their molecular structure: a four-atom ring known as a beta-lactam (β-lactam) ring. Through hydrolysis, the enzyme lactamase breaks the β-lactam ring open, deactivating the molecule's antibacterial properties. Beta-lactam antibiotics are typically used to target a broad spectrum of gram-positive and gram-negative bacteria. Beta-lactamases produced by gram-negative bacteria are usually secreted, especially when antibiotics are present in the environment. Structure The structure of a '' Streptomyces'' serine β-lactamase (SBLs) is given by . The alpha-beta fold ...
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