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Avibactam Synthesis

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The emergence of inhibitor-resistant bacterial strains and also inefficient inhibitory activity of traditional β-lactam inhibitors against KPC enzyme, is inspiring the development of a variety of new non-β-lactam\β-lactamase inhibitors. The search for such inhibitors was started with the hope of preserving β-lactam activity. 4.1 Avibactam (NXL104) Avibactam is a novel, covalent, reversible β-lactamase inhibitor with more potent and broader spectrum of activity (relative to clavulanic acid, sulbactam and tazobactam) against ESBL, AmpC, KPC as well as some class D enzymes which are resistant to inhibition by currently available β-lactam/β-lactamase inhibitors (Fig.1) (7, 56-58). This synthetic inhibitor has little intrinsic antibacterial activity …show more content…

It has been paired with two of third-generation cephalosporins, ceftazidime and ceftaroline. Ceftazidime alone is hydrolyzed by KPC enzyme, ESBLs and class C enzymes, but avibactam restores the antibacterial activity and also susceptibility of ceftazidime(60). Several studies were conducted to evaluate ceftazidime-avibactam combination. Data showed that this combination has better inhibitory activity than ceftazidime alone and is a valuable alternative to overcome Gram-negative bacilli including Enterobacteriacae, K.pneumoniae, E.cloacae and Burkholderia cefacian that produce class A carbapenemases and also majority of OXA-48 group of carbapenemases (61-66). However, ceftazidime-avibactam resistance have been demonstrated from KPC-2 variants such as KPC-3 producer Enterobacteriacae including K.pneumoniae and E.cloacae(67-69). Among β-lactamases, KPC-2 slowly hydrolyze avibactam(57, 68). Ceftazidime-avibactam has no activity against MBLs but because monobactams are not hydrolyzed by MBLs, aztreonam-avibactam combination is effective in vitro against MBL-producing Enterobacteriacae, especially NDM-producers that coproduce ESBLs or AmpC enzymes (56, …show more content…

Data from in vitro study has demonstrated that relebactam /imipenem combination is synergistic and shows considerably reduced MIC in imipenem-resistant isolates of KPC-producing K.pneumoniae and Pseudomonas strain (81-83). In a study that was conducted to evaluate the efficacy of relebactam-imipenem combination, relebactam restored 97% susceptibility of imipenem against KPC-producer K.pneumoniae isolates(84). Although MBLs(IMP, NDM, VIM) are not susceptible to relebactam /imipenem, OXA-48 producing Enterobacteriacae are weakly affected by this combination(70, 85). Due to greater potency of imipenem relative to cephalosporins, relebactam /imipenem combination is a better choice than ceftazidime-avibactam and ceftaroline-avibactam

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Gram positive organisms are susceptible to antibiotics such as penicillin (Introduction to Penicillins, 2012). This is because, gram positive bacteria have a thick layer of peptidoglycan, a sugar and peptide coating that gives a cell its shape and helps it stay intact (Wiley, 2004). The original antibiotic, penicillin, and the likes are used to treat infections caused by bacteria that are gram positive. Based on the scope of the experiment and the materials needed, a budget estimate of $1,000.00 would be needed to buy reagents and materials for this experiment.

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This antibiotic produced a zone of inhibition of 26mm and was therefore sensitive. After a little bit more research it was concluded that K. oxytoca produces B-lactamase, therefore making it resistant to penicillin and ampicillin (MicrobeWiki, 2015). Now that testing has been done the providers know what type of medication would be best to start with. Two out of four medications could possibly be used to attack the infection. If the patient were to take Ciprofloxacin the mechanism of action would be to inhibit relaxation of DNA; inhibit DNA gyrase in

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This experiment was tested on two conditions: +pGLO and -pGLO. +pGLO has the plasmid and -pGLO does not have the plasmid. Along with those conditions, ampicillin is added in the agar plate to destroy the non-transformed cells because scientist want to select only the transformed bacterial cells and the experiment is efficient at ten percent. To resist the antibiotic, the bacteria needs Beta lactamase that provide the enzyme. This allows the bacterial to break down the antibiotic and grow and with the plasmid.

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This led to the development and use of a penicillinase resistant beta-lactam antibiotic, including oxacillin and flucloxacillin. Combination therapy with gentamicin can also be used to treat more serious infections, but it can have a high risk of kidney

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Our hypothesis was that if the plate contains only the LB broth the E. coli bacteria would have no antibiotic resistance and would not glow. If the plate contains just LB broth and ampicillin then the E. coli bacteria will have antibiotic resistance only if the plasmid is present. If the plate contains LB broth, ampicillin and arabinose then the E. coli bacteria will glow fluorescent under a UV light and it will have antibiotic resistance. Similar to our expectations our results suggested that our hypothesis was correct. This is due to the fact that n order for the E coli.

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Penicillin, is the first antibiotic that is medically used to fight off a large range of bacterial infection. For this experiment, we will be using ampicillin, it is a part of the penicillin drug group. The ampicillin inhibits the bacteria with the result of killing the bacterium or prevents it from multiplying. “When a bacterium multiplies, small holes open up in their cell walls as the daughter cells divide.

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After 48 hours, I observed different growth patterns around the disks. I measured the zone of inhibition of each antibiotic and document them on Microbiology task 3

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Toluene was added to each tube in order to make holes in the E. coli cell membrane which killed all of the bacteria preventing any further changes in beta-galactosidase levels. 2.5 ml of 5% lactose was added to the E. coli mixture grown in glycerol only. Once lactose was added, 2ml of the mixture was added to the tube labeled with 0 min. The remaining E. coli mixture was put in a 37°C shaking water bath and a timer was started. After 5 minutes, the mixture was taken out of the shaker and added to the test tube labeled with 5 min.

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The Kirby-Bauer test is standardized in order to allow others to be able to reproduce the test since there are many factors that could affect the zone of inhibition. One of the standardizations is the medium used for the test, a Mueller-Hinton agar, which is different from the general mediums used in laboratories. The Mueller-Hinton agar plate is larger in size than standard agar plates so that multiple types of antibiotics are able to fit without interfering with each other (Slonczewski & Foster, 2015). The medium is thicker in depth (5 mm) and contains loose agar, which allows the antibiotics to diffuse out of the disk and into the media because if this test was conducted on a thinly poured agar plate, then the zone of inhibition would appear larger than it really is (Slonczewski & Foster, 2015). Another important factor about the Mueller-Hinton agar is that it doesn’t contain para-aminobenzoic (PABA) acid, which is usually present in most mediums.

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coli were seen. The bacterial cells’ ability to survive the ampicillin in the medium was a result of their transformation. As mentioned previously, the pGLO plasmid contained the beta-lactamase enzyme which is needed for antibiotic resistance. Since the E. coli on this plate underwent the transformation, they were able to uptake the beta-lactamase enzyme thereby making the bacterial cells ampicillin resistant. As well as being able to successfully grow and reproduce, the E. coli in the LB/amp/ara +pGLO plate also emitted a fluorescent glow when exposed to UV light.

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We thought that Penicillium was not inhibited because of structural differences between it and the susceptible fungi, but it is possible that penicillin killed off the bacteria. Unfortunately, the short stay prevented us from confirming our theory, and I left Costa Rica, longing for an extended research

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Unfortunately, carbapenem antibiotics often are the last line of defense against Gram-negative infections that are resistant to other antibiotics.

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Increasing incidences of antibiotic resistance among pathogens has created a demand to explore alternative treatment approaches. One such approach involves evaluating plant derived compounds for their activity against drug resistant pathogens. This study aims at examining the effect of green tea leaf extracts (GTE) on Metallo-β-lactamase (MBL) producing gram negative uropathogens. An ethanolic extract of GTE was prepared using soxhlet apparatus and its effect was studied on seven gram negative MBL producing uropathogens with respect to its Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC). In addition, the synergistic activity of ampicillin (a β-lactam drug) with GTE was carried out by agar dilution method to analyze the reduction in MBC of ampicillin in the presence of sub-lethal concentrations of GTE.

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This is where the antibacterial disc bacitracin was used to determine the bacteria’s susceptibility.

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