Lactams: Cyclic AMIDES formed from aminocarboxylic acids by the elimination of water. Lactims are the enol forms of lactams.Cyclization: Changing an open-chain hydrocarbon to a closed ring. (McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)Anti-Bacterial Agents: Substances that reduce the growth or reproduction of BACTERIA.beta-Lactams: Four-membered cyclic AMIDES, best known for the PENICILLINS based on a bicyclo-thiazolidine, as well as the CEPHALOSPORINS based on a bicyclo-thiazine, and including monocyclic MONOBACTAMS. The BETA-LACTAMASES hydrolyze the beta lactam ring, accounting for BETA-LACTAM RESISTANCE of infective bacteria.alpha-MSH: A 13-amino acid peptide derived from proteolytic cleavage of ADRENOCORTICOTROPIC HORMONE, the N-terminal segment of ACTH. ACTH (1-13) is amidated at the C-terminal to form ACTH (1-13)NH2 which in turn is acetylated to form alpha-MSH in the secretory granules. Alpha-MSH stimulates the synthesis and distribution of MELANIN in MELANOCYTES in mammals and MELANOPHORES in lower vertebrates.Antibiotic Prophylaxis: Use of antibiotics before, during, or after a diagnostic, therapeutic, or surgical procedure to prevent infectious complications.Heterocyclic Compounds, 1-Ring: A class of organic compounds containing a ring structure made up of more than one kind of atom, usually carbon plus another atom. The ring structure can be aromatic or nonaromatic.Microbial Sensitivity Tests: Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses).Muramic Acids: Compounds consisting of glucosamine and lactate joined by an ether linkage. They occur naturally as N-acetyl derivatives in peptidoglycan, the characteristic polysaccharide composing bacterial cell walls. (From Dorland, 28th ed)Streptomyces: A genus of bacteria that form a nonfragmented aerial mycelium. Many species have been identified with some being pathogenic. This genus is responsible for producing a majority of the ANTI-BACTERIAL AGENTS of practical value.Aminoglycosides: Glycosylated compounds in which there is an amino substituent on the glycoside. Some of them are clinically important ANTIBIOTICS.Molecular Structure: The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.Stereoisomerism: The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)Cyclacillin: A cyclohexylamido analog of PENICILLANIC ACID.Penicillins: A group of antibiotics that contain 6-aminopenicillanic acid with a side chain attached to the 6-amino group. The penicillin nucleus is the chief structural requirement for biological activity. The side-chain structure determines many of the antibacterial and pharmacological characteristics. (Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p1065)Drug Resistance, Bacterial: The ability of bacteria to resist or to become tolerant to chemotherapeutic agents, antimicrobial agents, or antibiotics. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).Amination: The creation of an amine. It can be produced by the addition of an amino group to an organic compound or reduction of a nitro group.Cleome: A plant genus of the family CAPPARACEAE that contains cleogynol and 15alpha-acetoxycleomblynol (dammaranes) and 1-epibrachyacarpone (a triterpene), and ISOTHIOCYANATES.Drug Resistance, Microbial: The ability of microorganisms, especially bacteria, to resist or to become tolerant to chemotherapeutic agents, antimicrobial agents, or antibiotics. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).Receptors, Melanocortin: A family of G-protein-coupled receptors that have specificity for MELANOCYTE-STIMULATING HORMONES and ADRENOCORTICOTROPIC HORMONE. There are several subtypes of melanocortin receptors, each having a distinct ligand specificity profile and tissue localization.Antibiotics, Antineoplastic: Chemical substances, produced by microorganisms, inhibiting or preventing the proliferation of neoplasms.Macrolides: A group of often glycosylated macrocyclic compounds formed by chain extension of multiple PROPIONATES cyclized into a large (typically 12, 14, or 16)-membered lactone. Macrolides belong to the POLYKETIDES class of natural products, and many members exhibit ANTIBIOTIC properties.Cephalosporins: A group of broad-spectrum antibiotics first isolated from the Mediterranean fungus ACREMONIUM. They contain the beta-lactam moiety thia-azabicyclo-octenecarboxylic acid also called 7-aminocephalosporanic acid.Streptothricins: A group of antibiotic aminoglycosides differing only in the number of repeating residues in the peptide side chain. They are produced by Streptomyces and Actinomyces and may have broad spectrum antimicrobial and some antiviral properties.Magnetic Resonance Spectroscopy: Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).Penicillin Resistance: Nonsusceptibility of an organism to the action of penicillins.Bacteria: One of the three domains of life (the others being Eukarya and ARCHAEA), also called Eubacteria. They are unicellular prokaryotic microorganisms which generally possess rigid cell walls, multiply by cell division, and exhibit three principal forms: round or coccal, rodlike or bacillary, and spiral or spirochetal. Bacteria can be classified by their response to OXYGEN: aerobic, anaerobic, or facultatively anaerobic; by the mode by which they obtain their energy: chemotrophy (via chemical reaction) or PHOTOTROPHY (via light reaction); for chemotrophs by their source of chemical energy: CHEMOLITHOTROPHY (from inorganic compounds) or chemoorganotrophy (from organic compounds); and by their source for CARBON; NITROGEN; etc.; HETEROTROPHY (from organic sources) or AUTOTROPHY (from CARBON DIOXIDE). They can also be classified by whether or not they stain (based on the structure of their CELL WALLS) with CRYSTAL VIOLET dye: gram-negative or gram-positive.Superinfection: A frequent complication of drug therapy for microbial infection. It may result from opportunistic colonization following immunosuppression by the primary pathogen and can be influenced by the time interval between infections, microbial physiology, or host resistance. Experimental challenge and in vitro models are sometimes used in virulence and infectivity studies.Bacterial Infections: Infections by bacteria, general or unspecified.IminesPeptides, Cyclic: Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).Gentamicins: A complex of closely related aminoglycosides obtained from MICROMONOSPORA purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit PROTEIN BIOSYNTHESIS.Bacterial Proteins: Proteins found in any species of bacterium.Structure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.Drug Utilization: The utilization of drugs as reported in individual hospital studies, FDA studies, marketing, or consumption, etc. This includes drug stockpiling, and patient drug profiles.Aza CompoundsAlkenes: Unsaturated hydrocarbons of the type Cn-H2n, indicated by the suffix -ene. (Grant & Hackh's Chemical Dictionary, 5th ed, p408)Drug Design: The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include pharmacokinetics, dosage analysis, or drug administration analysis.Carboxylic Acids: Organic compounds containing the carboxy group (-COOH). This group of compounds includes amino acids and fatty acids. Carboxylic acids can be saturated, unsaturated, or aromatic.Fermentation: Anaerobic degradation of GLUCOSE or other organic nutrients to gain energy in the form of ATP. End products vary depending on organisms, substrates, and enzymatic pathways. Common fermentation products include ETHANOL and LACTIC ACID.Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.Chromatography, Paper: An analytical technique for resolution of a chemical mixture into its component compounds. Compounds are separated on an adsorbent paper (stationary phase) by their varied degree of solubility/mobility in the eluting solvent (mobile phase).Escherichia coli: A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.Amides: Organic compounds containing the -CO-NH2 radical. Amides are derived from acids by replacement of -OH by -NH2 or from ammonia by the replacement of H by an acyl group. (From Grant & Hackh's Chemical Dictionary, 5th ed)Ampicillin: Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic.PeptidoglycanTetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.Staphylococcus aureus: Potentially pathogenic bacteria found in nasal membranes, skin, hair follicles, and perineum of warm-blooded animals. They may cause a wide range of infections and intoxications.Molecular Conformation: The characteristic three-dimensional shape of a molecule.Drug Resistance, Multiple, Bacterial: The ability of bacteria to resist or to become tolerant to several structurally and functionally distinct drugs simultaneously. This resistance may be acquired through gene mutation or foreign DNA in transmissible plasmids (R FACTORS).Gram-Positive Bacteria: Bacteria which retain the crystal violet stain when treated by Gram's method.Kanamycin: Antibiotic complex produced by Streptomyces kanamyceticus from Japanese soil. Comprises 3 components: kanamycin A, the major component, and kanamycins B and C, the minor components.Drug Therapy, Combination: Therapy with two or more separate preparations given for a combined effect.Bicyclo Compounds, Heterocyclic: A class of saturated compounds consisting of two rings only, having two or more atoms in common, containing at least one hetero atom, and that take the name of an open chain hydrocarbon containing the same total number of atoms. (From Riguady et al., Nomenclature of Organic Chemistry, 1979, p31)Anti-Infective Agents: Substances that prevent infectious agents or organisms from spreading or kill infectious agents in order to prevent the spread of infection.Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.Pseudomonas aeruginosa: A species of gram-negative, aerobic, rod-shaped bacteria commonly isolated from clinical specimens (wound, burn, and urinary tract infections). It is also found widely distributed in soil and water. P. aeruginosa is a major agent of nosocomial infection.Streptomycin: An antibiotic produced by the soil actinomycete Streptomyces griseus. It acts by inhibiting the initiation and elongation processes during protein synthesis.Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.Gram-Negative Bacteria: Bacteria which lose crystal violet stain but are stained pink when treated by Gram's method.Indium Radioisotopes: Unstable isotopes of indium that decay or disintegrate emitting radiation. In atoms with atomic weights 106-112, 113m, 114, and 116-124 are radioactive indium isotopes.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
  • 6 Of the three pharmacodynamic parameters described with antimicrobials, optimal efficacy with beta-lactams is achieved when free drug concentrations stay above the minimum inhibitory concentration (MIC) for an extended duration of the recommended dosing interval ( FIGURE 1 ). (uspharmacist.com)
  • Thus, strategies analogous to those implemented for Gram-negative pathogens are required to restore the efficacy of β-lactam antibiotics against Gram-positive pathogens such as MRSA. (sciencemag.org)
  • The critical pharmacodynamic parameter for antibacterial efficacy of β -lactam antibiotics is the proportion of the dosing interval for which the serum concentration of the non-protein-bound fraction of the antibiotic remains above its minimal inhibitory concentration (MIC) vis à vis the targeted pathogen. (ahcmedia.com)
  • If it is extraordinarily high, the duration of infusion is likely to be irrelevant - the antibiotic has little chance of efficacy. (ahcmedia.com)
  • The study was designed to investigate the safety and efficacy of DAV132, taken along with antibiotic treatment, to protect the intestinal microbiota. (davolterra.com)
  • In efforts to restore the efficacy of β-lactam antibiotics, β-lactamases have also been targeted with a variety of inhibitors ( 5 , 6 ). (pnas.org)
  • To this day, the pharmacology of beta-lactam antibiotics has clearly bore out an excellent safety and efficacy profile. (pharmafactz.com)
  • This study will assess the efficacy and safety of intravenous beta-lactam, in comparison with ceftriaxone, in hospitalized patients with community-acquired pneumonia not caused by Legionel. (bioportfolio.com)
  • This is a list of common β-lactam antibiotics-both administered drugs and those not in clinical use-organized by structural class. (wikipedia.org)
  • HS to β-lactams was suspected from clinical history in 30 (9.2%) children reporting serum sickness-like reactions and potentially harmful toxidermias. (aappublications.org)
  • Of the children diagnosed as allergic to β-lactam by means of skin tests, OC, and clinical history, 11.7% were sensitized to several classes of β-lactams. (aappublications.org)
  • NYSE MKT: SYN), a clinical stage company focused on developing therapeutics to protect the gut microbiome while targeting pathogen specific diseases, announced positive topline results from the first Phase 2a study of SYN-004, the Company's candidate designed to protect the gut microbiome from the unintended effects of certain commonly used intravenous (IV) beta-lactam antibiotics for the prevention C. (thefreedictionary.com)
  • In studies comparing the same beta-lactam, we observed no difference between study groups with regard to all-cause fatality, RR 1.01 (95% CI 0.75-1.35) and clinical failure, RR 1.11 (95% CI 0.95-1.29). (nih.gov)
  • In studies comparing different beta-lactams, we observed an advantage to monotherapy: all cause fatality RR 0.85 (95% CI 0.71-1.01), clinical failure RR 0.77 (95% CI 0.69-0.86). (nih.gov)
  • We found that low levels of β-lactam antibiotics, a class commonly used in both clinical and agricultural settings, caused significant autoaggregation and biofilm formation by the important human pathogen Staphylococcus aureus. (nih.gov)
  • CONCLUSIONS: Continuous administration of beta-lactam antibiotics achieved higher plasma antibiotic concentrations than intermittent administration with improvement in clinical cure. (biomedsearch.com)
  • Mechanisms responsible for resistance to β-Iactam antibiotics were investigated in clinical isolates of Bacteroides spp. (nottingham.ac.uk)
  • The results suggest that several different types of resistance to β-lactam antibiotics are circulating in clinical isolates of Bacteroides spp. (nottingham.ac.uk)
  • Unlike organotropic drugs, where it is easy to titrate dose to achieve a clinical response, antibiotics may take 24-72 h to present signs of resolution of infection, making it difficult to determine the most appropriate dosage [ 1 , 2 ]. (biomedcentral.com)
  • V ardakas and colleagues examined 22 clinical trials involving 1,876 patients prescribed intravenous anti-pseudomonal β -lactam antibiotics and who were randomized to receive them either as a brief (over ≤ 60 minutes) or prolonged ( ≥ 3 hours, including continuous) infusion. (ahcmedia.com)
  • Paris (France), 1st of September, 2020 - Da Volterra, a clinical-stage biopharmaceutical company developing innovative products to protect the intestinal microbiota from the deleterious effects of antibiotics, announced positive results from DAV132-CL-1006, a Phase 1 clinical study which investigated the effect of two doses of DAV132 in healthy volunteers receiving ß-lactam antibiotics. (davolterra.com)
  • We are delighted with the results of this Phase 1 study which provides the first clinical demonstration of the ability of DAV132 to spare the intestinal microbiota from the dysbiosis caused by ß-lactam antibiotics. (davolterra.com)
  • The study is of tremendous importance as ß-lactams are widely used in clinical practice and are known to be one of the main drivers for the emergence, in the intestinal microbiota, of pathogenic species such as C. difficile, as well as for the selection of antibiotic-resistant pathogens. (davolterra.com)
  • This is a multi-center, randomized, double-blind, placebo-controlled, superiority clinical trial evaluating short course (5 day) vs. standard course (10 day) of oral beta-lactam antibiotic therapy (amoxicillin, amoxicillin-clavulanate, cefdinir) for treatment of CAP in children 6-71 months of age who have clinically improved prior to enrollment. (clinicaltrials.gov)
  • 1,000 growth/killing curves for eight combinations of antibiotics and bacterial species and strains, including clinical isolates of bacterial pathogens. (pnas.org)
  • As new β-lactams have been introduced into clinical use, a changing landscape of β-lactamases has been selected and disseminated. (pnas.org)
  • The three inhibitors approved for clinical use are clavulanic acid, tazobactam, and sulbactam, all of which contain a β-lactam core. (pnas.org)
  • STUDY SELECTION AND DATA EXTRACTION: Randomized controlled clinical trials, pharmacokinetic/pharmacodynamic studies, observational studies, and case reports involving pediatric patients who received extended or continuous infusion of b-lactam or monobactam antibiotics were reviewed. (elsevier.com)
  • There is limited clinical evidence available to support the use of extended or continuous infusion of b-lactam antibiotics in the pediatric population. (elsevier.com)
  • CONCLUSIONS: More well-designed prospective clinical trials are required to determine the role of extended or continuous infusion of b-lactam antibiotics in treatment of pediatric patients. (elsevier.com)
  • As part of our commitment to fight antimicrobial resistance through minimizing the environmental impact from antibiotics manufacturing, DSP is actively seeking to promote green, enzymatic routes for production of amoxicillin and other antibiotics, utilizing our patented technology. (medindia.net)
  • Knowledge of the antimicrobial PD characteristics (inhibition of growth, rate and extent of bactericidal action, and post-antibiotic effect (PAE)) provides a more rational basis for determination of optimal dosing regimens in terms of the dose and the dosing interval. (biomedcentral.com)
  • From previous studies performed in our laboratories, it is believed that the N-thiolated beta-lactams exert their antimicrobial activity through a unique mode of action that is completely unlike that of classical beta-lactam antibiotics. (usf.edu)
  • Typically when an antibiotic is applied to the agar medium, it moves from its region of high concentration to the surrounding areas of lower antimicrobial concentration (Cooper, 1993, p.24). (studentshare.org)
  • We demonstrate that GlcEnt-Amp/Amx provide up to 1000-fold enhanced antimicrobial activity against uropathogenic E. coli relative to the parent β-lactams. (rsc.org)
  • A 2.0 Å crystal structure of S. aureus FtsZ in complex with PC190723 identifies the compound binding site, which corresponds to the predominant location of mutations conferring resistance to PC190723 (PC190723 R ). Although structural studies suggested that these drug resistance mutations may be difficult to combat through chemical modification of PC190723, combining PC190723 with the β-lactam antibiotic imipenem markedly reduced the spontaneous frequency of PC190723 R mutants. (sciencemag.org)
  • In these trials, no differences between single and combination antibiotic treatments were seen. (cochrane.org)
  • This linear dependence of the lysis rate on the growth rate represents a dynamic signature associated with each bacterium-antibiotic pair and serves as the quantitative foundation for designing combination antibiotic therapy and predicting the population-structure change in a population with mixed phenotypes. (pnas.org)
  • Further, the effect of TC and EG on the expression of A. baumannii genes encoding resistance to β-lactam antibiotics ( blaP ), efflux pumps ( adeABC ), and multi-drug resistant protein ( mdrp ) was studied using real-time quantitative PCR (RT-qPCR). (frontiersin.org)
  • Inactivation of genes coding for components of these systems was also shown to decrease the MICs of some β-lactams. (asm.org)
  • Most of the samples yielded β-lactam-resistant isolates, and 4 different groups of bla genes were detected among the isolates. (springer.com)
  • Antibiotic residues can adversely affect bacterial starter cultures used in the production of milk-based products such as cheese and yoghurts. (dcu.ie)
  • The specificity of these antibodies was determined and they were used in displacement immunoassays for the detection of the relevant antibiotic in 'spiked' samples of PBS and whole milk. (dcu.ie)
  • The article also reviews recent data suggesting increased overall mortality with Cefepime (Maxipime) use compared with other beta-lactam antibiotics and the potential risk for neurotoxicity in the setting of renal failure. (journaltocs.info)
  • In the first chapter of this dissertation, a review of previously prepared N-thiolated beta-lactam analogues and their mode of action is presented. (usf.edu)