Synthesis and properties of bioactive surfactants containing β-lactam ring

Author(s):  
L. Molina ◽  
M. J. Stébé ◽  
C. Selve ◽  
A. Perani ◽  
M. Maugras ◽  
...  
Keyword(s):  
2020 ◽  
Vol 16 (4) ◽  
pp. 456-464
Author(s):  
Danilo F. Rodrigues ◽  
Hérida R.N. Salgado

Background: A simple, eco-friendly and low-cost Infrared (IR) method was developed and validated for the analysis of Cefepime Hydrochloride (CEF) in injectable formulation. Different from some other methods, which employ organic solvents in the analyses, this technique does not use these types of solvents, removing large impacts on the environment and risks to operators. Objective: This study aimed at developing and validating a green analytical method using IR spectroscopy for the determination of CEF in pharmaceutical preparations. Methods: The method was validated according to ICH guidelines and the quantification of CEF was performed in the spectral region absorbed at 1815-1745 cm-1 (stretching of the carbonyl group of β- lactam ring). Results: The validated method showed to be linear (r = 0.9999) in the range of 0.2 to 0.6 mg/pellet of potassium bromide, as well as for the parameters of selectivity, precision, accuracy, robustness and Limits of Detection (LOD) and Quantification (LOQ), being able to quantify the CEF in pharmaceutical preparations. The CEF content obtained by the IR method was 103.86%. Conclusion: Thus, the method developed may be an alternative in the quality control of CEF sample in lyophilized powder for injectable solution, as it presented important characteristics in the determination of the pharmaceutical products, with low analysis time and a decrease in the generation of toxic wastes to the environment.


2021 ◽  
Vol 6 (7) ◽  
pp. 1705-1709
Author(s):  
Mireille F. Kemgni ◽  
Laurice Bracine N. Chenda ◽  
Joseph Tchamgoue ◽  
Patrice T. Kenfack ◽  
Yvan Anderson T. Ngandjui ◽  
...  
Keyword(s):  

Antibiotics ◽  
2021 ◽  
Vol 10 (3) ◽  
pp. 298
Author(s):  
Alexander Ecke ◽  
Rudolf J. Schneider

Contamination of waters with pharmaceuticals is an alarming problem as it may support the evolution of antimicrobial resistance. Therefore, fast and cost-effective analytical methods for potential on-site analysis are desired in order to control the water quality and assure the safety of its use as a source of drinking water. Antibody-based methods, such as the enzyme-linked immunosorbent assay (ELISA), can be helpful in this regard but can also have certain pitfalls in store, depending on the analyte. As shown here for the class of β-lactam antibiotics, hydrolysis of the β‑lactam ring is a key factor in the immunochemical analysis as it influences antibody recognition. With the antibody used in this study, the limit of detection (LOD) in the immunoassay could be significantly reduced by hydrolysis for the five tested penicillins, with the lowest LOD for carbenicillin (0.2 nmol/L) and the greatest impact on penicillins G and V (reduction by 85%). In addition to enhanced quantification, our strategy also provides access to information about the degree of hydrolysis in water samples as shown for the most abundant penicillin amoxicillin.


ChemInform ◽  
2010 ◽  
Vol 25 (32) ◽  
pp. no-no
Author(s):  
Y. KITA ◽  
N. SHIBATA ◽  
N. YOSHIDA ◽  
N. KAWANO ◽  
K. MATSUMOTO

1980 ◽  
Vol 1 (7) ◽  
pp. 197-201
Author(s):  
Michael J. Kraemer ◽  
Arnold L. Smith

Ampicillin, first introduced in 1961, has probably become the most widely used penicillin in clinical pediatrics. STRUCTURE ACTIVITY RELATIONSHIPS All penicillins contain the 6-amino penicillanic acid moiety (Fig 1). Its structure includes a thiazolidine ring (A), a β-lactam ring (B), the source of antibacterial activity, and an acyl side chain (R), containing a variety of substitutions creating the family of semisynthetic penicillins. The only difference between ampicillin and penicillin G is the presence of an amino group in the acyl side chain (Fig 1). PHARMACOLOGY AND BACTERIOLOGY Ampicillin is a semisynthetic penicillin, active against Streptococus pneumoniae and certain Gram-negative bacteria, including most Haemophilus influenzae, Escherichia coli, and certain Proteus species. Compared to penicillin G, it has increased stability in acid solutions: a property facilitating oral administration and absorption. It penetrates into most body tissues; effective entry into CSF, however, occurs only with inflamed meninges. The serum half-life with normal renal function varies from four hours in newborns1 to 1.3 hours in adults.2 Ampicillin can cause an allergic, or nonallergic skin rash (Fig 2). ALLERGY Allergy (for the purposes of this discussion) is defined as a specific immunologic interaction, between either antigen and antibody, or antigen with a sensitized lymphocyte, resulting in a clinically deleterious effect. Implicit is a prior contact with the antigen.


Author(s):  
Kavi Aniis ◽  
Rajamanikandan Kcp ◽  
Arvind Prasanth D

<p>ABSTRACT<br />Objective: Beta-lactams are the group of antibiotics that contain a ring called as “beta-lactam ring,” which is responsible for the antibacterial activity.<br />The presence of resistance among Gram-negative organisms is due to the production of beta-lactamases enzymes that hydrolysis the beta-lactam ring<br />thereby conferring resistance to the organism. This study is undertaken to determine the prevalence of extended-spectrum beta-lactamase (ESBL)<br />producing Gram-negative organism from clinical samples.<br />Methods: A total of 112 clinical samples were taken for this study. The combined disc synergistic test (CDST) was used for the phenotypic detection<br />of ESBL producers from the clinical samples. The genotypic identification of ESBL producers was carried out by alkaline lysis method by isolation of<br />plasmid DNA.<br />Result: A total of 87 bacterial isolates were isolated and identified. Among them, Klebsiella (41%) was the predominant organism followed by<br />Escherichia coli (33%), Proteus (10%), Pseudomonas (10%), and Serratia (6%). Among the various bacterial isolates, Klebsiella showed a higher<br />percentage of resistance. The CDST showed that 8 isolates of Klebsiella, 3 isolates of E. coli, and 1 isolate of Pseudomonas were found to be ESBL<br />producers. The genotypic confirmation showed that the two bacterial isolates, namely, Klebsiella and E. coli were found to possess temoniera (TEM)<br />gene which was the 400-500 bp conferring resistance to the antibiotics.<br />Conclusion: The results of this study suggest that early detection of ESBL producing Gram-negative organism is a very important step in planning the<br />therapy of patient in Hospitals. CDST continues to be a good indicator in the detection of ESBL producers.<br />Keywords: Beta-lactamases, Gram-negative bacilli, Extended-spectrum beta-lactamase, Resistance, Combined disc synergistic test.</p><p> </p>


Synthesis ◽  
2018 ◽  
Vol 50 (23) ◽  
pp. 4539-4554 ◽  
Author(s):  
Javier Vicario ◽  
Francisco Palacios ◽  
Edorta Martinez de Marigorta ◽  
Jesús de los Santos ◽  
Ana Ochoa de Retana

This review summarizes the synthesis of γ-lactam ring using multicomponent reactions.1 Introduction2 Pyrrolidin-2-ones3 Pyrrolin-2-ones (Dihydro-2H-pyrrol-2-ones)4 Final Remarks


2021 ◽  
Vol 37 (2) ◽  
pp. 113-125
Author(s):  
M.K Salihu ◽  
A Yarima ◽  
H.I Atta

1983. These enzymes possess the ability to inactivate susceptible β-lactam antibiotics i.e. penicillins, first, second and third generation cephalosporins and aztreonam, but not cephamycins and carbapenems . Their mode of action is by hydrolyzing the β-lactam ring. Even before the first β-lactam antibiotic (penicillin) was developed, resistance to β-lactam antibiotics was observed . ESBL genes are plasmids- and transposons- mediated, as such, can be spread easily to other species of bacteria. Resistance of ESBL- producing bacteria to the β-lactam antibiotics is a continuing cause of public health problems , it is increasingly being observed in community and nosocomial acquired infections. Detection and identification of these ESBLs in the laboratory is of prime importance for the selection of appropriate antibiotics to be used in the treatment of infections caused by ESBL- producing bacteria. The aim of this review is to explain in detail , several phenotypic methods used in the detection and confirmation of extended spectrum β lactamases. Keywords: Antibiotic resistance, ESBL, bacteria, phenotypic method


1999 ◽  
Vol 341 (2) ◽  
pp. 409-413 ◽  
Author(s):  
Noureddine RHAZI ◽  
Moreno GALLENI ◽  
Michael I. PAGE ◽  
Jean-Marie FRÈRE

Although β-lactamases have generally been considered as being devoid of peptidase activity, a low but significant hydrolysis of various N-acylated dipeptides was observed with representatives of each class of β-lactamases. The kcat/Km values were below 0.1 M-1˙s-1, but the enzyme rate enhancement factors were in the range 5000-20000 for the best substrates. Not unexpectedly, the best ‘peptidase’ was the class C β-lactamase of Enterobacter cloacae P99, but, more surprisingly, the activity was always higher with the phenylacetyl- and benzoyl-D-Ala-D-Ala dipeptides than with the diacetyl- and α-acetyl-L-Lys-D-Ala-D-Ala tripeptides, which are the preferred substrates of the low-molecular-mass, soluble DD-peptidases. A comparison between the β-lactamases and DD-peptidases showed that it might be as difficult for a DD-peptidase to open the β-lactam ring as it is for the β-lactamases to hydrolyse the peptides, an observation which can be explained by geometric and stereoelectronic considerations.


2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Edurne Peña-Mendizabal ◽  
Sergi Morais ◽  
Ángel Maquieira

Abstract New antigens deriving from -lloyl and -llanyl, major and minor determinants, respectively, were produced for β-lactam antibiotics cefuroxime, cefotaxime, ceftriaxone, meropenem and aztreonam. Twenty β-lactam antigens were produced using human serum albumin and histone H1 as carrier proteins. Antigens were tested by multiplex in vitro immunoassays and evaluated based on the detection of specific IgG and IgE in the serum samples. Both major and minor determinants were appropriate antigens for detecting specific anti-β-lactam IgG in immunised rabbit sera. In a cohort of 37 allergic patients, we observed that only the minor determinants (-llanyl antigens) were suitable for determining specific anti-β-lactam IgE antibodies with high sensitivity (< 0.01 IU/mL; 24 ng/L) and specificity (100%). These findings reveal that not only the haptenisation of β-lactam antibiotics renders improved molecular recognition events when the 4-member β-lactam ring remains unmodified, but also may contribute to develop promising minor antigens suitable for detecting specific IgE-mediated allergic reactions. This will facilitate the development of sensitive and selective multiplexed in vitro tests for drug-allergy diagnoses to antibiotics cephalosporin, carbapenem and monobactam.


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