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Journal articles on the topic 'Lactam Based Molecules'

Author: Grafiati

Published: 6 September 2023

Last updated: 31 July 2025

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1

Bai, Yuchen, Leina Dou, Weilin Wu та ін. "Anti-Metatype Antibody Screening, Sandwich Immunoassay Development, and Structural Insights for β-Lactams Based on Penicillin Binding Protein". Molecules 26, № 18 (2021): 5569. http://dx.doi.org/10.3390/molecules26185569.

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Theoretically, sandwich immunoassay is more sensitive and has a wider working range than that of competitive format. However, it has been thought that small molecules cannot be detected by the sandwich format due to their limited size. In the present study, we proposed a novel strategy for achieving sandwich immunoassay of β-lactams with low molecular weights. Firstly, five β-lactam antibiotics were selected to bind with penicillin binding protein (PBP)2x* to form complexes. Then, monoclonal and polyclonal antibodies against PBP2x*-β-lactams complexes were produced by animal immunization. Subs

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2

Becker, D., M. Botoshansky, N. Gasper, F. H. Herbstein, and M. Karni. "2-Phenyl-4-hydroxyphthalazin-1-one: A Benzoannelated Derivative of Maleic Hydrazide." Acta Crystallographica Section B Structural Science 54, no. 5 (1998): 671–76. http://dx.doi.org/10.1107/s0108768197015760.

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The monoclinic crystals (space group P21/a, Z = 8) of 2-phenyl-4-hydroxyphthalazin-1-one, C14H10N2O2, have two independent molecules (A and B) in the asymmetric unit. Both occur as the lactim–lactam (hydroxy–one) structure, which is also found in the parent molecule maleic hydrazide (both triclinic and monoclinic polymorphs), dichloromaleic hydrazide and luminol (3-aminophthalhydrazide). The molecular arrangement is based on strings of alternating A and B molecules linked by hydroxyl...carbonyl hydrogen bonds, with only van der Waals interactions between adjacent strings. Comparison is made of

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Cox, Robin A. "Lactams in sulfuric acid. The mechanism of amide hydrolysis in weak to moderately strong aqueous mineral acid media." Canadian Journal of Chemistry 76, no. 6 (1998): 649–56. http://dx.doi.org/10.1139/v98-012.

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Reaction rate constants obtained in moderately concentrated sulfuric acid for the hydrolysis of simple lactams of ring sizes five, six, seven, and eight as a function of acidity and temperature have been analyzed using the excess acidity kinetic method. The basicity constants for these substrates have been recalculated; the 13C NMR spectra used to obtain these values are very sensitive to medium effects. It was found that the basicities of the lactams at 0.003-0.1 M lactam concentration were over half a pK unit more basic than they were at 0.5 M lactam, presumably because of the medium effect.

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4

Pestana-Nobles, Roberto, Yani Aranguren-Díaz, Elwi Machado-Sierra, et al. "Docking and Molecular Dynamic of Microalgae Compounds as Potential Inhibitors of Beta-Lactamase." International Journal of Molecular Sciences 23, no. 3 (2022): 1630. http://dx.doi.org/10.3390/ijms23031630.

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Bacterial resistance is responsible for a wide variety of health problems, both in children and adults. The persistence of symptoms and infections are mainly treated with β-lactam antibiotics. The increasing resistance to those antibiotics by bacterial pathogens generated the emergence of extended-spectrum β-lactamases (ESBLs), an actual public health problem. This is due to rapid mutations of bacteria when exposed to antibiotics. In this case, β-lactamases are enzymes used by bacteria to hydrolyze the beta-lactam rings present in the antibiotics. Therefore, it was necessary to explore novel m

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Molteni, Elena, Giovanni Onida, Matteo Ceccarelli, and Giancarlo Cappellini. "Ab Initio Spectroscopic Investigation of Pharmacologically Relevant Chiral Molecules: The Cases of Avibactam, Cephems, and Idelalisib as Benchmarks for Antibiotics and Anticancer Drugs." Symmetry 13, no. 4 (2021): 601. http://dx.doi.org/10.3390/sym13040601.

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The ability to accurately measure or predict several physicochemical properties of molecules which play a role as active substances in drugs can be of strategic importance for pharmacological applications, in addition to its possible interest in fundamental research. Chirality is a relevant feature in the characterization of drug molecules: enantiomers can show different pharmacological activity and adverse effects. The ability to separate stereoisomers and to assign their absolute configuration can thus be crucial. Circular dichroism (CD) spectra are a useful tool to distinguish between enant

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Twamley, Brendan, Niamh M. O'Boyle, and Mary J. Meegan. "Azetidin-2-ones: structures of antimitotic compounds based on the 1-(3,4,5-trimethoxyphenyl)azetidin-2-one core." Acta Crystallographica Section E Crystallographic Communications 76, no. 8 (2020): 1187–94. http://dx.doi.org/10.1107/s2056989020008555.

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A series of related substituted 1-(3,4,5-trimethoxyphenyl)azetidin-2-ones have been characterized: 3-(4-fluorophenyl)-4-(4-methoxyphenyl)-1-(3,4,5-trimethoxyphenyl)azetidin-2-one, C25H24FNO5 (1), 3-(furan-2-yl)-4-(4-methoxyphenyl)-1-(3,4,5-trimethoxyphenyl)azetidin-2-one, C23H23NO6 (2), 4-(4-methoxyphenyl)-3-(naphthalen-1-yl)-1-(3,4,5-trimethoxyphenyl)azetidin-2-one, C29H27NO5 (3), 3-(3,4-dimethoxyphenyl)-4-(4-methoxyphenyl)-1-(3,4,5-trimethoxyphenyl)azetidin-2-one, C27H29NO7 (4) and 4,4-bis(4-methoxyphenyl)-3-phenyl-1-(3,4,5-trimethoxyphenyl)azetidin-2-one, C32H31NO6 (5). All of the compounds

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7

Shiri, Pezhman. "Novel Hybrid Molecules Based on triazole-β-lactam as Potential Biological Agents". Mini-Reviews in Medicinal Chemistry 21, № 5 (2021): 536–53. http://dx.doi.org/10.2174/18755607mtewaotyn5.

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8

Kurmaz, Svetlana V., Natalia V. Fadeeva, Vladislav M. Ignat’ev, Vladimir A. Kurmaz, Sergei A. Kurochkin, and Nina S. Emel’yanova. "Structure and State of Water in Branched N-Vinylpyrrolidone Copolymers as Carriers of a Hydrophilic Biologically Active Compound." Molecules 25, no. 24 (2020): 6015. http://dx.doi.org/10.3390/molecules25246015.

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Hydrated copolymers of N-vinylpyrrolidone (VP) with triethylene glycol dimethacrylate as a promising platform for biologically active compounds (BAC) were investigated by different physical chemical methods (dynamic light scattering, infrared spectroscopy, thermal gravimetric analysis, and differential scanning calorimetry) and the quantum chemical modeling of water coordination by the copolymers in a solution. According to the quantum chemical simulation, one to two water molecules can coordinate on one O-atom of the lactam ring of VP units in the copolymer. Besides the usual terminal coordin

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9

Shlaes, D. M., та C. Currie-McCumber. "Mutations altering substrate specificity in OHIO-1, and SHV-1 family β-lactamase". Biochemical Journal 284, № 2 (1992): 411–15. http://dx.doi.org/10.1042/bj2840411.

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The OHIO-1 beta-lactamase does not normally hydrolyse oxyimino-beta-lactam substrates like cefotaxime, ceftriaxone, ceftazidime or aztreonam. We were able to select spontaneous mutants of an OHIO-1-bearing strain of Escherichia coli using the antibiotic substrates listed above by enrichment methods of frequencies of 10(-8)-10(-10) for all antibiotics except ceftazidime (frequency less than 10(-10)). Most mutants with increased resistance to the other beta-lactams were also more resistant to ceftazidime. Mutations identified by DNA sequencing included a Gly238----Ser238 substitution identical w

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10

Maity, Arindam, Sarmi Sardar, Shilpa Chatterjee, Nripendra Nath Bala, Sudhan Debnath та Debanjan Sen. "De-Novo Design of Hits Against New Delhi Metallo-β-Lactamase Enzyme". International Journal of Quantitative Structure-Property Relationships 7, № 2 (2022): 1–13. http://dx.doi.org/10.4018/ijqspr.290010.

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The New Delhi Metallo-β-lactamase 1 (NDM-1) is a class of Metallo-β lactamase enzyme. It is responsible for hydrolyzing almost all β-lactam antibiotics, leading to multi-drug resistance in bacteria. The lack of specific therapeutic options against this target creates an emerging need to develop new molecules against it. The multistep fragment- and knowledge-based de-novo design methods were considered for this study to design small molecules. The designed molecules were evaluated by molecular docking and dynamics simulation, followed by drug-likeness prediction. This study reports that a new d

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11

Khalesi, Maryam, Azim Ziyaei Halimehjani, and Jürgen Martens. "Synthesis of a novel category of pseudo-peptides using an Ugi three-component reaction of levulinic acid as bifunctional substrate, amines, and amino acid-based isocyanides." Beilstein Journal of Organic Chemistry 15 (April 4, 2019): 852–57. http://dx.doi.org/10.3762/bjoc.15.82.

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The synthesis of a novel category of pseudo-peptides via intramolecular Ugi reaction of levulinic acid (4-oxopentanoic acid), aromatic and aliphatic amines, and amino acid-based isocyanides is reported. Levulinic acid was applied as a bifunctional substrate containing both carbonyl and acid moieties suitable for the Ugi reaction. This article provides a facile and convenient one-pot procedure for the synthesis of peptide-like heterocyclic molecules containing 2-pyrrolidone (γ-lactam), amide and ester functional groups with good to excellent yields.

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12

M. Al-Maaqar, Saleh, Bassam O. Al-Johny, Fahdah Ayed Alshammari, et al. "IDENTIFICATION OF ANTIBACTERIAL AGENTS AGAINST KLEBSIELLA PNEUMONIAE TARGETING THE CTX-M-15 PROTEIN USING INTEGRATED STRUCTURE MODEL-BASED VIRTUAL SCREENING METHODS." Journal of microbiology, biotechnology and food sciences 14, no. 2 (2024): e11876. http://dx.doi.org/10.55251/jmbfs.11876.

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The spread of carbapenem-resistant Gram-negative bacteria, particularly those having the bla CTX-M-15 gene, has stimulated a global challenge for β-lactam antimicrobial effectiveness. This study aims to identify commercially available compounds that demonstrate strong antibacterial properties with high efficacy and low toxicity to combat the increasing problem of antibiotic resistance. Virtual screening and molecular docking techniques were employed to generate a pharmacophore model based on the molecular structure. Eleven potential compounds were selected based on their IC50 values. Subsequen

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13

Lourenço, Ana Laura Pereira, Thuanny Borba Rios, Állan Pires da Silva, Octávio Luiz Franco, and Marcelo Henrique Soller Ramada. "Peptide Stapling Applied to Antimicrobial Peptides." Antibiotics 12, no. 9 (2023): 1400. http://dx.doi.org/10.3390/antibiotics12091400.

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Antimicrobial peptides (AMPs) are considered a promising therapeutic approach against multi-drug resistant microorganisms. Besides their advantages, there are limitations to be overcome so that these molecules can become market competitive. One of the biggest limitations is proteolytic susceptibility, which could be overcome by structural modifications such as cyclization, especially for helix-constraining strategies. Over the years, many helix stabilization techniques have arisen, such as lactam-bridging, triazole-based, N-alkylation and all-hydrocarbon stapling. All-hydrocarbon stapling take

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14

Abdullah, Shahla M., та Shwan Rachid. "On Column Binding a Real-Time Biosensor for β-lactam Antibiotics Quantification". Molecules 25, № 5 (2020): 1248. http://dx.doi.org/10.3390/molecules25051248.

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This work aimed to develop accurate, quick, and practical tools for the detection of residues of penicillin G antibiotic in biological and non-biological samples. The assays were developed based on the binding mechanism of β-lactam to penicillin-binding proteins; samples of different concentrations of penicillin G were incubated with in vitro expressed 6X-Histidine-tagged soluble penicillin-binding protein (PBP2x*) of Streptococcus pneumoniae (S. pneumoniae), whereby penicillin G in samples specifically binds to PBP2x*. The fluorescent-labeled β-lactam analogue Bocillin FL was used as a compet

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15

Minhas, Gurdeep S., and Simon Newstead. "Structural basis for prodrug recognition by the SLC15 family of proton-coupled peptide transporters." Proceedings of the National Academy of Sciences 116, no. 3 (2019): 804–9. http://dx.doi.org/10.1073/pnas.1813715116.

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A major challenge in drug development is the optimization of intestinal absorption and cellular uptake. A successful strategy has been to develop prodrug molecules, which hijack solute carrier (SLC) transporters for active transport into the body. The proton-coupled oligopeptide transporters, PepT1 and PepT2, have been successfully targeted using this approach. Peptide transporters display a remarkable capacity to recognize a diverse library of di- and tripeptides, making them extremely promiscuous and major contributors to the pharmacokinetic profile of several important drug classes, includi

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16

Ferková, Sára, Ulrike Froehlich, Marie-Édith Nepveu-Traversy, et al. "Comparative Analysis of Cyclization Techniques in Stapled Peptides: Structural Insights into Protein–Protein Interactions in a SARS-CoV-2 Spike RBD/hACE2 Model System." International Journal of Molecular Sciences 25, no. 1 (2023): 166. http://dx.doi.org/10.3390/ijms25010166.

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Medicinal chemistry is constantly searching for new approaches to develop more effective and targeted therapeutic molecules. The design of peptidomimetics is a promising emerging strategy that is aimed at developing peptides that mimic or modulate the biological activity of proteins. Among these, stapled peptides stand out for their unique ability to stabilize highly frequent helical motifs, but they have failed to be systematically reported. Here, we exploit chemically diverse helix-inducing i, i + 4 constraints—lactam, hydrocarbon, triazole, double triazole and thioether—on two distinct shor

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17

Vladimirov, Sergey Alimovich, Gleb Dmitrievich Rukhovich, Eugene Valerievich Radchenko, and Irina Vasilievna Perminova. "DEVELOPMENT OF APPROACHES TO MOLECULAR MODELING OF THE INTERACTION OF BIOLOGICALLY ACTIVE COMPONENTS OF HUMIC SUBSTANCES WITH BETA-LACTAMASES ON THE EXAMPLE OF HUMIC-LIKE LOW-MOLECULAR WEIGHT ANALOGUES." chemistry of plant raw material, no. 2 (June 17, 2024): 329–39. https://doi.org/10.14258/jcprm.20240213955.

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β-Lactamase inhibitors are used to protect betalactam antibiotics from the action of antibiotic resistant bacteria. However, due to the emergence of resistance to β-lactam inhibitors, the search for new non-betalactam inhibitors is an urgent task. In this work, natural humic substances (HS) are considered as a new source of beta-lactamase inhibitors. We previously reported on the ability of coal humic acids and their narrow fractions to inhibit TEM-1 β-lactamases. The purpose of this work was to study the mechanism of interaction between the molecular components of humic substances using molec

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18

Lánská, B., L. Matisová-Rychlá, J. Broz̆ek, and J. Rychlý. "Chemiluminescence of polyamides II. Luminescence accompanying thermooxidation of lactam-based polyamides related to the content of end-groups of molecules." Polymer Degradation and Stability 66, no. 3 (1999): 433–44. http://dx.doi.org/10.1016/s0141-3910(99)00096-8.

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Chepak, Aleksandr, Denis Balatskiy, Mikhail Tutov, Aleksandr Mironenko, and Svetlana Bratskaya. "Light Harvesting Nanoprobe for Trace Detection of Hg2+ in Water." Molecules 28, no. 4 (2023): 1633. http://dx.doi.org/10.3390/molecules28041633.

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The continuously increasing flow of toxic heavy metals to the environment due to intensive industrial activity and tightening requirements with regard to the content of metal ions in drinking and discharged waters urges the development of affordable and sensitive devices to the field control of pollutants. Here, we report a new thiated Rhodamine-lactam probe for Hg2+ detection and demonstrate how its sensitivity can be increased via the incorporation of the probe molecules into the optically transparent siloxane-acrylate coatings on polymethyl methacrylate and, alternatively, into the water-di

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20

Li, Shen, Ying Zhou, Yujuan Yan, Yinying Qin, Qilu Weng, and Litao Sun. "Structure-Based Virtual Screening, ADMET Properties Prediction and Molecular Dynamics Studies Reveal Potential Inhibitors of Mycoplasma pneumoniae HPrK/P." Life 14, no. 6 (2024): 657. http://dx.doi.org/10.3390/life14060657.

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Mycoplasma pneumoniae pneumonia (MPP) is a frequent cause of community-acquired pneumonia (CAP) in children. The incidence of childhood pneumonia caused by M. pneumoniae infection has been rapidly increasing worldwide. M. pneumoniae is naturally resistant to beta-lactam antibiotics due to its lack of a cell wall. Macrolides and related antibiotics are considered the optimal drugs for treating M. pneumoniae infection. However, clinical resistance to macrolides has become a global concern in recent years. Therefore, it is imperative to urgently identify new targets and develop new anti-M. pneumo

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Zarganes-Tzitzikas, Tryfon, Gonçalo Clemente, Philip Elsinga, and Alexander Dömling. "MCR Scaffolds Get Hotter with 18F-Labeling." Molecules 24, no. 7 (2019): 1327. http://dx.doi.org/10.3390/molecules24071327.

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Imaging techniques, such as positron emission tomography (PET), represent great progress in the clinical development of drugs and diagnostics. However, the efficient and timely synthesis of appropriately labeled compounds is a largely unsolved problem. Numerous small drug-like molecules with high structural diversity can be synthesized via convergent multicomponent reactions (MCRs). The combination of PET labeling with MCR synthesis of biologically active compounds can greatly simplify radioanalytical and imaging-based analysis. In a proof-of-concept study, we optimized robust on-site radiolab

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Presnova, Galina V., Denis E. Presnov, Anna A. Filippova, Ilia I. Tsiniaikin, Mariya M. Ulyashova та Maya Yu Rubtsova. "Multiplex Digital Quantification of β-Lactamase Genes in Antibiotic-Resistant Bacteria by Counting Gold Nanoparticle Labels on Silicon Microchips". Biosensors 12, № 4 (2022): 226. http://dx.doi.org/10.3390/bios12040226.

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Digital quantification based on counting of individual molecules is a promising approach for different biomedical applications due to its enhanced sensitivity. Here, we present a method for the digital detection of nucleic acids (DNA and RNA) on silicon microchips based on the counting of gold nanoparticles (GNPs) in DNA duplexes by scanning electron microscopy (SEM). Biotin-labeled DNA is hybridized with capture oligonucleotide probes immobilized on the microchips. Then biotin is revealed by a streptavidin–GNP conjugate followed by the detection of GNPs. Sharp images of each nanoparticle allo

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Maham Khan, Shahid Wahab, Haroon Muhammad Ali, Sadia Khan, Reema Iqbal, and Tariq Khan. "Biogenic Nanomaterials: A Way Forward in Preventing Bacterial Infections." Proceedings of the Pakistan Academy of Sciences: B. Life and Environmental Sciences 60, S (2023): 3–23. http://dx.doi.org/10.53560/ppasb(60-sp1)814.

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Antibiotic resistance puts a tremendous strain on the healthcare system. Bacteria such as Staphylococcus aureus, Klebsiella pneumoniae, and Pseudomonas aeruginosa that cause diseases like endocarditis, pneumonia, and Urinary tract infections have now become resistant to many previously used antibiotics. Antibiotic overuse must be reduced as it has become a public health threat paving the way to pandemics. Instead of creating new antibiotics, repurposing existing medicines that have faced resistance is one way forward. Plant-based antimicrobials have been explored as antibiotics to boost or aug

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Aslanli, Aysel, Ilya Lyagin, and Elena Efremenko. "Novel approach to quorum quenching: rational design of antibacterials in combination with hexahistidine-tagged organophosphorus hydrolase." Biological Chemistry 399, no. 8 (2018): 869–79. http://dx.doi.org/10.1515/hsz-2018-0162.

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Abstract N-acyl homoserine lactones (AHLs) are quorum sensing (QS) signal molecules used by most Gram-negative pathogenic bacteria. In this article the lactonase activity of the preparations based on hexahistidine-tagged organophosphorus hydrolase (His6-OPH) towards AHLs was studied. Initially, three of the most interesting β-lactam antibiotics were selected from seven that were trialed during molecular docking to His6-OPH. Combinations of antibiotics (meropenem, imipenem, ceftriaxone) and His6-OPH taken in the native form or in the form of non-covalent enzyme-polyelectrolyte complexes (EPCs)

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25

Gaudêncio, Susana P., and Florbela Pereira. "Predicting Antifouling Activity and Acetylcholinesterase Inhibition of Marine-Derived Compounds Using a Computer-Aided Drug Design Approach." Marine Drugs 20, no. 2 (2022): 129. http://dx.doi.org/10.3390/md20020129.

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Biofouling is the undesirable growth of micro- and macro-organisms on artificial water-immersed surfaces, which results in high costs for the prevention and maintenance of this process (billion €/year) for aquaculture, shipping and other industries that rely on coastal and off-shore infrastructure. To date, there are still no sustainable, economical and environmentally safe solutions to overcome this challenging phenomenon. A computer-aided drug design (CADD) approach comprising ligand- and structure-based methods was explored for predicting the antifouling activities of marine natural product

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Kamat, Shweta, Pankaj Gupta та Akshata Mane. "2288. Role of Β Lactam-Β Lactamase Inhibitors in Indian Tertiary Care Hospitals: Results from a Nationwide Survey". Open Forum Infectious Diseases 6, Supplement_2 (2019): S784. http://dx.doi.org/10.1093/ofid/ofz360.1966.

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Abstract Background Broad-spectrum antibiotics, particularly third-generation cephalosporins, are routinely used in the treatment of nosocomial infections. The emergence of Extended Spectrum Β-Lactamase (ESBL)-producing pathogens in Indian tertiary care hospitals warrants the need to reassess β-lactam–β-lactamase inhibitors (BL-BLIs) as better alternative treatments. Methods An online survey was conducted by Pfizer India to understand the usage of BL-BLIs across Indian hospitals. The survey was administered to 334 clinicians across multiple specialties out of which 195 were from tertiary care

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Alkhatabi, Heba Ahmed, та Hisham N. Alatyb. "Pharmacophore-Based Study: An In Silico Perspective for the Identification of Potential New Delhi Metallo-β-lactamase-1 (NDM-1) Inhibitors". Pharmaceuticals 17, № 9 (2024): 1183. http://dx.doi.org/10.3390/ph17091183.

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In the ongoing battle against antibiotic-resistant bacteria, New Delhi metallo-β-lactamase-1 (NDM-1) has emerged as a significant therapeutic challenge due to its ability to confer resistance to a broad range of β-lactam antibiotics. This study presents a pharmacophore-based virtual screening, docking, and molecular dynamics simulation approach for the identification of potential inhibitors targeting NDM-1, a critical enzyme associated with antibiotic resistance. Through the generation of a pharmacophore model and subsequent virtual screening of compound libraries, candidate molecules (ZINC291

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NIKOLAEV, A. YU, O. M. LAVROVA, R. G. TAGASHEVA, D. K. KOMUNAROVA, E. L. GAVRILOVA, and A. V. BOGDANOV. "SYNTHESIS OF HYBRID COMPOUNDS BASED ON ISATIN DERIVATIVES AND PHOSPHORYLCARBOXYLIC ACID HYDRAZIDES." Herald of Technological University 27, no. 8 (2024): 29–33. https://doi.org/10.55421/1998-7072_2024_27_8_29.

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The development of new biologically active substances and pharmaceuticals often involves the strategic combination of different pharmacophore elements into hybrid structures. Drugs created using this method may have increased efficacy, reduced toxicity and a multifaceted spectrum of biological action. Isatin is isolated as a synthetically versatile substance, often used in the creation of various heterocyclic structures. There are two active sites in its structure - a carbonyl group and a lactam segment, which makes isatin an excellent basis for the development of hybrid biologically active co

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Borgianni, Luisa, Julie Vandenameele, André Matagne та ін. "Mutational Analysis of VIM-2 Reveals an Essential Determinant for Metallo-β-Lactamase Stability and Folding". Antimicrobial Agents and Chemotherapy 54, № 8 (2010): 3197–204. http://dx.doi.org/10.1128/aac.01336-09.

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ABSTRACT Metallo-β-lactamase (MBL)-producing bacteria are emerging worldwide and represent a formidable threat to the efficacy of relevant β-lactams, including carbapenems, expanded-spectrum cephalosporins, and β-lactamase inactivator/β-lactam combinations. VIM-2 is currently the most widespread MBL and represents a primary target for MBL inhibitor research, the clinical need for which is expected to further increase in the future. Using a saturation mutagenesis approach, we probed the importance of four residues (Phe-61, Ala-64, Tyr-67, and Trp-87) located close to the VIM-2 active site and p

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Bhagwanth, Swapna, Ram K. Mishra, and Rodney L. Johnson. "Development of peptidomimetic ligands of Pro-Leu-Gly-NH2 as allosteric modulators of the dopamine D2 receptor." Beilstein Journal of Organic Chemistry 9 (January 30, 2013): 204–14. http://dx.doi.org/10.3762/bjoc.9.24.

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A variety of stable, small-molecule peptidomimetic ligands have been developed to elucidate the mechanism by which the neuropeptide Pro-Leu-Gly-NH2 (PLG) modulates dopaminergic neurotransmission. Photoaffinity labeling ligands based upon PLG peptidomimetics have been used to establish that PLG binds to the D2 dopamine receptor at a site that is different from the orthosteric site, thus making PLG and its peptidomimetics allosteric modulators of the dopamine receptor. Through the design, synthesis and pharmacological evaluation of conformationally constrained peptidomimetics containing lactam,

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Diarra, M. S., M. C. Lavoie, M. Jacques, et al. "Species selectivity of new siderophore-drug conjugates that use specific iron uptake for entry into bacteria." Antimicrobial Agents and Chemotherapy 40, no. 11 (1996): 2610–17. http://dx.doi.org/10.1128/aac.40.11.2610.

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Siderophores selectively bind ferric iron and are involved in receptor-specific iron transport into bacteria. Several types of siderophores were synthesized, and growth-promoting or inhibitory activities when they were conjugated to carbacephalosporin, erythromycylamine, or nalidixic acid were investigated. Overall, 11 types of siderophores and 21 drug conjugates were tested against seven different bacterial species: Escherichia coli, Bordetella bronchiseptica, Pasteurella multocida, Pasteurella haemolytica, Streptococcus suis, Staphylococcus aureus, and Staphylococcus epidermidis. In some spe

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Biswal, Sarmistha, Karina Caetano, Diamond Jain та ін. "Antimicrobial Peptides Designed against the Ω-Loop of Class A β-Lactamases to Potentiate the Efficacy of β-Lactam Antibiotics". Antibiotics 12, № 3 (2023): 553. http://dx.doi.org/10.3390/antibiotics12030553.

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Class A serine β-lactamases (SBLs) have a conserved non-active site structural domain called the omega loop (Ω-loop), in which a glutamic acid residue is believed to be directly involved in the hydrolysis of β-lactam antibiotics by providing a water molecule during catalysis. We aimed to design and characterise potential pentapeptides to mask the function of the Ω-loop of β-lactamases and reduce their efficacy, along with potentiating the β-lactam antibiotics and eventually decreasing β-lactam resistance. Considering the Ω-loop sequence as a template, a group of pentapeptide models were design

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Anant, Prem Singh, and Pratima Gupta. "Application of machine learning in understanding bioactivity of beta-lactamase AmpC." Journal of Physics: Conference Series 2273, no. 1 (2022): 012005. http://dx.doi.org/10.1088/1742-6596/2273/1/012005.

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Abstract The ability of microorganisms like bacteria to develop mechanisms against the treatment is becoming a concern globally. This topic of concern is called Antimicrobial Resistance aka AMR. In this study, with the help of machine learning algorithms we are trying to evaluate the activity of molecules that have been tested experimentally either to bind or not bind the beta lactamases. Machine learning is a technique for analysis of data which teaches the computers what naturally comes to living organisms. Beta lactamases are diverse family of microbial enzymes that hydrolyse the cyclic ami

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Innocent Allepo ABE, Flora YAO, Félix Kouadio YEBOUE, Barkissa TRAORE, Thomas KONAN, and Mathurin KOFFI. "Detection of genetic determinants of extended-spectrum beta-lactam resistance in Klebsiella pneumoniae and Escherichia coli strains from cattle feces in the Haut-Sassandra region, central-west of Côte d'Ivoire." GSC Advanced Research and Reviews 21, no. 3 (2024): 416–24. https://doi.org/10.30574/gscarr.2024.21.3.0509.

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As in human health, beta-lactams are widely used molecules in veterinary medicine for the treatment of bacterial infections. This study conducted in the Haut-Sassandra region of Côte d'Ivoire aims to investigate the extended-spectrum beta-lactamase resistance of Klebsiella pneumoniae and Escherichia coli strains isolated from cattle excrement. Fecal samples from cattle were collected in the Daloa and Zoukougbeu departments. Fifty cattle fecal samples were collected across the two departments, including thirty-six in Daloa and fourteen in Zoukougbeu. Bacterial cultures were performed on these f

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Sharan, Deepti, та Erin E. Carlson. "Expanded profiling of β-lactam selectivity for penicillin-binding proteins in Streptococcus pneumoniae D39". Biological Chemistry 403, № 4 (2022): 433–43. http://dx.doi.org/10.1515/hsz-2021-0386.

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Abstract Penicillin-binding proteins (PBPs) are integral to bacterial cell division as they mediate the final steps of cell wall maturation. Selective fluorescent probes are useful for understanding the role of individual PBPs, including their localization and activity during growth and division of bacteria. For the development of new selective probes for PBP imaging, several β-lactam antibiotics were screened, as they are known to covalently bind PBP in vivo. The PBP inhibition profiles of 16 commercially available β-lactam antibiotics were evaluated in an unencapsulated derivative of the D39

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Aslanli, Aysel, and Elena Efremenko. "Simultaneous molecular docking of different ligands to His6-tagged organophosphorus hydrolase as an effective tool for assessing their effect on the enzyme." PeerJ 7 (September 12, 2019): e7684. http://dx.doi.org/10.7717/peerj.7684.

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Background Enzymatic hydrolysis of N-acyl homoserine lactones (AHLs), which are signaling molecules responsible for the development of antibiotic resistance in gram-negative bacteria, is a potential solution to overcoming antibiotic resistance problem. It has been established that hexahistidine-tagged organophosphorus hydrolase (His6-OPH) exhibits lactonase activity against a number of AHLs and that the combined application of His6-OPH with β-lactam antibiotics leads to an increase in the efficiency of the action of both the enzyme and antibiotics. The use of computational methods can be an ef

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Yamada, Masanori, and Itaru Honma. "An Anhydrous Proton Conductor Based on Lactam–Lactim Tautomerism of Uracil." ChemPhysChem 5, no. 5 (2004): 724–28. http://dx.doi.org/10.1002/cphc.200301015.

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Flores, Anthony R., Linda M. Parsons та Martin S. Pavelka. "Characterization of Novel Mycobacterium tuberculosis and Mycobacterium smegmatis Mutants Hypersusceptible to β-Lactam Antibiotics". Journal of Bacteriology 187, № 6 (2005): 1892–900. http://dx.doi.org/10.1128/jb.187.6.1892-1900.2005.

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ABSTRACT Our laboratory previously constructed mutants of Mycobacterium tuberculosis and Mycobacterium smegmatis with deletions in the genes for their major β-lactamases, BlaC and BlaS, respectively, and showed that the mutants have increased susceptibilities to most β-lactam antibiotics, particularly the penicillins. However, there is still a basal level of resistance in the mutants to certain penicillins, and the susceptibilities of the mutants to some cephalosporin-based β-lactams are essentially the same as those of the wild types. We hypothesized that characterizing additional mutants (de

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Bobba, Sudheer, V. K. Chaithanya Ponnaluri, Mridul Mukherji, and William G. Gutheil. "Microtiter Plate-Based Assay for Inhibitors of Penicillin-Binding Protein 2a from Methicillin-Resistant Staphylococcus aureus." Antimicrobial Agents and Chemotherapy 55, no. 6 (2011): 2783–87. http://dx.doi.org/10.1128/aac.01327-10.

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ABSTRACTPenicillin-binding protein 2a (PBP2a), the molecular determinant for high-level β-lactam resistance in methicillin-resistantStaphylococcus aureus(MRSA), is intrinsically resistant to most β-lactam antibiotics. The development and characterization of new inhibitors targeting PBP2a would benefit from an effective and convenient assay for inhibitor binding. This study was directed toward the development of a fluorescently detected β-lactam binding assay for PBP2a from MRSA. Biotinylated ampicillin and biotinylated cephalexin were tested as tagging reagents for fluorescence detection by us

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Listro, Roberta, Giacomo Rossino, Serena Della Volpe та ін. "Enantiomeric Resolution and Absolute Configuration of a Chiral δ-Lactam, Useful Intermediate for the Synthesis of Bioactive Compounds". Molecules 25, № 24 (2020): 6023. http://dx.doi.org/10.3390/molecules25246023.

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During the past several years, the frequency of discovery of new molecular entities based on γ- or δ-lactam scaffolds has increased continuously. Most of them are characterized by the presence of at least one chiral center. Herein, we present the preparation, isolation and the absolute configuration assignment of enantiomeric 2-(4-bromophenyl)-1-isobutyl-6-oxopiperidin-3-carboxylic acid (trans-1). For the preparation of racemic trans-1, the Castagnoli-Cushman reaction was employed. (Semi)-preparative enantioselective HPLC allowed to obtain enantiomerically pure trans-1 whose absolute configura

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del Corte, Xabier, Adrián López-Francés, Ilia Villate-Beitia та ін. "Multicomponent Synthesis of Unsaturated γ-Lactam Derivatives. Applications as Antiproliferative Agents through the Bioisosterism Approach: Carbonyl vs. Phosphoryl Group". Pharmaceuticals 15, № 5 (2022): 511. http://dx.doi.org/10.3390/ph15050511.

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We report efficient synthetic methodologies for the preparation of 3-amino and 3-hydroxy 3-pyrrolin-2-ones (unsaturated γ-lactams) through a multicomponent reaction of amines, aldehydes and acetylene or pyruvate derivatives. The densely substituted γ-lactam substrates show in vitro cytotoxicity, inhibiting the growth of the carcinoma human tumor cell lines RKO (human colon epithelial carcinoma), SKOV3 (human ovarian carcinoma) and A549 (carcinomic human alveolar basal epithelial cell). In view of the possibilities for the diversity of the substituents that offer a multicomponent, synthetic met

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A. Ali, Fattma. "The Role of Virulence Factors of Haemophilus Influenza." Journal of Clinical Case Reports & Studies 6, no. 1 (2025): 01–05. https://doi.org/10.31579/2690-8808/237.

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Background: Haemophilus influenzae is a pathogenic bacterium that frequently leads to serious infections, especially in newborns. Haemophilus influenzae is a Gram-ve coccobacillus belonging to the Pasteurellaceae family. It is microscopic in size, ranging from 0.3 to 1 micrometers. Its facultative anaerobic can survive with or without oxygen and has the ability to change its shape. It grows in an environment with increased levels of carbon dioxide. The development of this organism on chocolate agar is facilitated by a medium that contains two erythrocyte factors: factor X (hematin) and factor

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Shkutina, Irina V., Natalia V. Mironenko, and Vladimir F. Selemenev. "Sorption processes in the "6-methyluracil-super-cross-linked polymer" system." Сорбционные и хроматографические процессы 23, no. 3 (2023): 360–72. http://dx.doi.org/10.17308/sorpchrom.2023.23/11316.

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The study presents the results of investigation of the processes of sorption of 6-methyluracil (MU) by low basic anion exchanger A-100 and high basic anion exchanger A-500R, which have a macroporous structure. It was found that the maximum sorption was observed at pH 3.2-3.5; in the area when 6-methyluracil (6-methyl-2.4-dioxo-pyrimidine) was in the lactam form in the solution. The obtained sorption isotherms were analysed. It was noted that the formation of monomolecular layers of 6-methyluracil (MU) on A-100 and A-500R ion exchangers can be described by the Langmuir isotherm equation. With a

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Pathompong, Paomephan, Sebastian Pfütze, Frank Surup, et al. "Drimane-Type Sesquiterpenoids Derived from the Tropical Basidiomycetes Perenniporia centrali-africana and Cerrena sp. nov." Molecules 27, no. 18 (2022): 5968. http://dx.doi.org/10.3390/molecules27185968.

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Five new drimane-type sesquiterpenoids were isolated from cultures of the tropical basidiomycetes, Perenniporia centrali-africana (originating from Kenya) and Cerrena sp. nov. (originating from Thailand). A new pereniporin A derivative (1), a new drimane-type sesquiterpene lactam (2), and the new 6,7-Dehydro-isodrimenediol (3) were isolated from P. centrali-africana. In parallel, the two new drimane-type sesquiterpene lactams 5 and 6 were isolated together with known isodrimenediol (4) from Cerrena sp. This is the first report of drimane-type sesquiterpene lactams from basidiomycetes. The stru

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Collia, Deanna, Thomas D. Bannister, Hao Tan та ін. "A Rapid Phenotypic Whole-Cell Screening Approach for the Identification of Small-Molecule Inhibitors That Counter β-Lactamase Resistance in Pseudomonas aeruginosa". SLAS DISCOVERY: Advancing the Science of Drug Discovery 23, № 1 (2017): 55–64. http://dx.doi.org/10.1177/2472555217728489.

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Pseudomonas aeruginosa is an opportunistic human pathogen that is prevalent in hospitals and continues to develop resistance to multiple classes of antibiotics. Historically, β-lactam antibiotics have been the first line of therapeutic defense. However, the emergence of multidrug-resistant (MDR) strains of P. aeruginosa, such as AmpC β-lactamase overproducing mutants, limits the effectiveness of current antibiotics. Among AmpC hyperproducing clinical isolates, inactivation of AmpG, which is essential for the expression of AmpC, increases bacterial sensitivity to β-lactam antibiotics. We hypoth

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Ambade, Shraddha S., Vivek Kumar Gupta, Ritesh P. Bhole, Pramod B. Khedekar, and Rupesh V. Chikhale. "A Review on Five and Six-Membered Heterocyclic Compounds Targeting the Penicillin-Binding Protein 2 (PBP2A) of Methicillin-Resistant Staphylococcus aureus (MRSA)." Molecules 28, no. 20 (2023): 7008. http://dx.doi.org/10.3390/molecules28207008.

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Staphylococcus aureus is a common human pathogen. Methicillin-resistant Staphylococcus aureus (MRSA) infections pose significant and challenging therapeutic difficulties. MRSA often acquires the non-native gene PBP2a, which results in reduced susceptibility to β-lactam antibiotics, thus conferring resistance. PBP2a has a lower affinity for methicillin, allowing bacteria to maintain peptidoglycan biosynthesis, a core component of the bacterial cell wall. Consequently, even in the presence of methicillin or other antibiotics, bacteria can develop resistance. Due to genes responsible for resistan

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Liu, Xinyu, Shengjie Dong, Yuru Ma, Hu Xu, Hongxia Zhao та Qingzhi Gao. "N-(Sulfamoylbenzoyl)-L-proline Derivatives as Potential Non-β-lactam ESBL Inhibitors: Structure-Based Lead Identification, Medicinal Chemistry and Synergistic Antibacterial Activities". Medicinal Chemistry 15, № 2 (2019): 196–206. http://dx.doi.org/10.2174/1573406414666180816123232.

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Background: There is an urgent need to develop novel inhibitors against clinically widespread extended-spectrum β-lactamases (ESBLs) to meet the challenges of the ever-evolving threat of antibiotic resistances. Most existing ESBL inhibitors sharing a common chemical feature of β-lactam ring in their molecule, this structural characteristic makes them intrinsically susceptible to enzymatic breakdown by the resistance mechanisms employed by the bacteria. Objective: The aim of this study was to screen and discover novel lead compounds by using Lproline as initial scaffold to create a “non-sulfur,

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Ahmadvand, Parvaneh, Johannetsy J. Avillan, Jacob A. Lewis, Douglas R. Call, and ChulHee Kang. "Characterization of Interactions between CTX-M-15 and Clavulanic Acid, Desfuroylceftiofur, Ceftiofur, Ampicillin, and Nitrocefin." International Journal of Molecular Sciences 23, no. 9 (2022): 5229. http://dx.doi.org/10.3390/ijms23095229.

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Cefotaximase-Munich (CTX-M) extended-spectrum beta-lactamases (ESBLs) are commonly associated with Gram-negative, hospital-acquired infections worldwide. Several beta-lactamase inhibitors, such as clavulanate, are used to inhibit the activity of these enzymes. To understand the mechanism of CTX-M-15 activity, we have determined the crystal structures of CTX-M-15 in complex with two specific classes of beta-lactam compounds, desfuroylceftiofur (DFC) and ampicillin, and an inhibitor, clavulanic acid. The crystal structures revealed that Ser70 and five other residues (Lys73, Tyr105, Glu166, Ser13

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Liang, Lujie, Lan-Lan Zhong, Lin Wang та ін. "A new variant of the colistin resistance gene MCR-1 with co-resistance to β-lactam antibiotics reveals a potential novel antimicrobial peptide". PLOS Biology 21, № 12 (2023): e3002433. http://dx.doi.org/10.1371/journal.pbio.3002433.

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The emerging and global spread of a novel plasmid-mediated colistin resistance gene, mcr-1, threatens human health. Expression of the MCR-1 protein affects bacterial fitness and this cost correlates with lipid A perturbation. However, the exact molecular mechanism remains unclear. Here, we identified the MCR-1 M6 variant carrying two-point mutations that conferred co-resistance to β-lactam antibiotics. Compared to wild-type (WT) MCR-1, this variant caused severe disturbance in lipid A, resulting in up-regulation of L, D-transpeptidases (LDTs) pathway, which explains co-resistance to β-lactams.

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Shiri, Pezhman. "Novel hybrid molecules based on triazole-β-lactam as potential biological agents". Mini-Reviews in Medicinal Chemistry 20 (27 жовтня 2020). http://dx.doi.org/10.2174/1389557520666201027160436.

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: Triazole ring is a cyclic scaffold containing three heteroatoms of nitrogen. They display a broad variety of biological activities. The uncatalyzed/catalyzed 1,3‐dipolar cycloadditions are a chemical reaction between a 1,3-dipole and a dipolarophile to achieve 1,2,3‐triazoles. The hybrid approach is an innovative and powerful synthetic tool for the synthesis of two or more distinct entities in one molecule with novel biological activities. Owing to the high potential of β-lactams to display noticeable biological properties, these compounds have been one of the important ingredients in hybrid

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