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Infectious Disease Clinics of North... Jun 2000Experimental animal models have provided information applicable to antimicrobial therapy of infections of the central nervous system. The efficacy of an antimicrobial... (Review)
Review
Experimental animal models have provided information applicable to antimicrobial therapy of infections of the central nervous system. The efficacy of an antimicrobial agent in the therapy of bacterial meningitis depends on its ability to penetrate the blood-brain barrier, its activity in purulent cerebrospinal fluid, and a demonstration of rapid bactericidal activity against the offending pathogen. The recent emergence of resistant pathogens is challenging the therapy for bacterial meningitis. Various strategies for treating resistant pathogens have been evaluated in experimental animal models. Encouraging results have led to clinical trials to evaluate the efficacy of newer agents, alone or in combination with standard regimens.
Topics: Animals; Anti-Bacterial Agents; Cerebrospinal Fluid; Humans; Meningitis, Bacterial
PubMed: 10829262
DOI: 10.1016/s0891-5520(05)70254-3 -
Mikrobiyoloji Bulteni Apr 2010The continuously increasing problem of multidrug-resistant (extended-spectrum beta-lactamase and/or metallo-beta-lactamase producing) bacteria in recent years has... (Review)
Review
The continuously increasing problem of multidrug-resistant (extended-spectrum beta-lactamase and/or metallo-beta-lactamase producing) bacteria in recent years has created the need to re-evaluate antibiotic therapy for these infections. Fosfomycin is reconsidered to be an alternative treatment agent for such infections. Fosfomycin was first discovered in Spain in 1969 from cultures of Streptomyces species and originally called phosphonomycin. In the early years, fosfomycin was administered parenterally to the patients with many serious infections including meningitis. In some European countries, fosfomycin is occasionally administered for the initial empirical therapy of sepsis or soft-tissue infections. Although in most European countries fosfomycin has been used for many years, it has become available in clinical use only recently in Turkey. In USA, the Food and Drug Administration (FDA) has approved fosfomycin only for the treatment of patients with uncomplicated cystitis. The use of fosfomycin in the treatment of multidrug-resistant bacterial infections and in the treatment of pediatric cancer patients with fever and neutropenia in combination with other antibiotics, has withdrawn attention to this agent. Fosfomycin has a rapid bactericidal effect and a wide antibacterial spectrum, including methicillin-resistant Staphylococcus aureus, glycopeptide-susceptible or resistant enterococci and a large number of gram-negative pathogens. Since it has a long serum half-life and high concentrations are achieved in urine after oral administration; fosfomycin deserved further consideration for single-dose treatment of urinary tract infections caused by Escherichia coil and Enterococcus faecalis. In this review article the properties, mechanisms of action and resistance, antibacterial spectrum, clinical use, toxicity and adverse reactions of fosfomycin have been summarized.
Topics: Anti-Bacterial Agents; Enterococcus faecalis; Escherichia coli Infections; Fosfomycin; Gram-Positive Bacterial Infections; History, 20th Century; History, 21st Century; Humans; Urinary Tract Infections
PubMed: 20549968
DOI: No ID Found -
Chemistry, An Asian Journal Sep 2008Actinopyrone A, an anti-Helicobacter pylori agent, was synthesized in nine steps from a silyl dienol ether. A vinylogous anti-aldol was stereoselectively synthesized by...
Actinopyrone A, an anti-Helicobacter pylori agent, was synthesized in nine steps from a silyl dienol ether. A vinylogous anti-aldol was stereoselectively synthesized by our developed remote stereoinduction methodology; coupling of this with a sulfone and a phosphonate species led to the construction of a vinylpyrone compound. This was submitted to reductive de-conjugation to give actinopyrone A. The absolute stereochemistry of actinopyrone A was determined to have the configuration 14R,15R.
Topics: Anti-Bacterial Agents; Helicobacter pylori; Models, Molecular; Molecular Structure; Pyrones
PubMed: 18633953
DOI: 10.1002/asia.200800109 -
Journal of Global Antimicrobial... Sep 2020The increasing crisis regarding multidrug-resistant (MDR) and extensively drug-resistant microorganisms leads to appealing therapeutic options. (Review)
Review
OBJECTIVES
The increasing crisis regarding multidrug-resistant (MDR) and extensively drug-resistant microorganisms leads to appealing therapeutic options.
METHODS
During the last 30 years, minocycline, a wide-spectrum antimicrobial agent, has been effective against MDR Gram-positive and Gram-negative bacterial infections. As with other tetracyclines, the mechanism of action of minocycline involves attaching to the bacterial 30S ribosomal subunit and preventing protein synthesis.
RESULTS
This antimicrobial agent has been approved for the treatment of acne vulgaris, some sexually transmitted diseases and rheumatoid arthritis. Although many reports have been published, there remains limited information regarding the prevalence, mechanism of resistance and clinical effectiveness of minocycline.
CONCLUSION
Thus, we summarize here the currently available data concerning pharmacokinetics and pharmacodynamics, mechanism of action and resistance, antibacterial activity and clinical effectiveness of minocycline.
Topics: Acne Vulgaris; Anti-Bacterial Agents; Anti-Infective Agents; Gram-Negative Bacterial Infections; Humans; Minocycline
PubMed: 32061815
DOI: 10.1016/j.jgar.2020.01.022 -
The Journal of the Dental Association... Nov 1994Although clindamycin is not the drug of first choice for the majority of orofacial infections, it has a definite place in dental therapeutics. The pharmacology of this... (Review)
Review
Although clindamycin is not the drug of first choice for the majority of orofacial infections, it has a definite place in dental therapeutics. The pharmacology of this agent and its use in clinical dentistry is discussed in this review.
Topics: Anti-Bacterial Agents; Bacterial Infections; Clindamycin; Dental Care; Drug Resistance, Microbial; Humans; Mouth Diseases
PubMed: 9508961
DOI: No ID Found -
Bioorganic & Medicinal Chemistry Dec 2016With the emergence of multidrug-resistant bacterial strains, there is a dire need for new drug targets for antibacterial drug discovery and development. Filamentous... (Review)
Review
With the emergence of multidrug-resistant bacterial strains, there is a dire need for new drug targets for antibacterial drug discovery and development. Filamentous temperature sensitive protein Z (FtsZ), is a GTP-dependent prokaryotic cell division protein, sharing less than 10% sequence identity with the eukaryotic cell division protein, tubulin. FtsZ forms a dynamic Z-ring in the middle of the cell, leading to septation and subsequent cell division. Inhibition of the Z-ring blocks cell division, thus making FtsZ a highly attractive target. Various groups have been working on natural products and synthetic small molecules as inhibitors of FtsZ. This review summarizes the recent advances in the development of FtsZ inhibitors, focusing on those in the last 5years, but also includes significant findings in previous years.
Topics: Anti-Bacterial Agents; Bacteria; Bacterial Proteins; Cytoskeletal Proteins; Drug Discovery; Humans; Microbial Sensitivity Tests; Structure-Activity Relationship
PubMed: 27189886
DOI: 10.1016/j.bmc.2016.05.003 -
Drugs & Aging Jul 2017Surgical site infections are among the most common healthcare-associated infections and are linked with increased length of hospitalization, re-admission, mortality and... (Review)
Review
Surgical site infections are among the most common healthcare-associated infections and are linked with increased length of hospitalization, re-admission, mortality and significant financial burden. Risk factors for the occurrence of surgical site infections include variables related to the surgical procedure as well as host factors. Increasing age is associated with the occurrence of surgical site infections. The aim of this review is to give an update on the antibiotic prophylaxis for surgical site infection in elderly people. We focused on specific issues and practical applications, such as the importance of targeting the antimicrobial agent to the susceptibility pattern of colonizing flora in selected cases and the need for dosage modifications.
Topics: Aged; Anti-Bacterial Agents; Antibiotic Prophylaxis; Dose-Response Relationship, Drug; Drug Administration Schedule; Humans; Risk Factors; Surgical Wound Infection
PubMed: 28589466
DOI: 10.1007/s40266-017-0471-9 -
Mayo Clinic Proceedings Jun 1999In addition to erythromycin, macrolides now available in the United States include azithromycin and clarithromycin. These two new macrolides are more chemically stable... (Review)
Review
In addition to erythromycin, macrolides now available in the United States include azithromycin and clarithromycin. These two new macrolides are more chemically stable and better tolerated than erythromycin, and they have a broader antimicrobial spectrum than erythromycin against Mycobacterium avium complex (MAC), Haemophilus influenzae, nontuberculous mycobacteria, and Chlamydia trachomatis. All three macrolides have excellent activity against the atypical respiratory pathogens (C. pneumoniae and Mycoplasma species) and the Legionella species. Azithromycin and clarithromycin have pharmacokinetics that allow shorter dosing schedules because of prolonged tissue levels. Both azithromycin and clarithromycin are active agents for MAC prophylaxis in patients with late-stage acquired immunodeficiency syndrome (AIDS), although azithromycin may be the preferable agent because of fewer drug-drug interactions. Clarithromycin is the most active MAC antimicrobial agent and should be part of any drug regimen for treating active MAC disease in patients with or without AIDS. Although both azithromycin and clarithromycin are well tolerated by children, azithromycin has the advantage of shorter treatment regimens and improved tolerance, potentially improving compliance in the treatment of respiratory tract and skin or soft tissue infections. Intravenously administered azithromycin has been approved for treatment of adults with mild to moderate community-acquired pneumonia or pelvic inflammatory diseases. An area of concern is the increasing macrolide resistance that is being reported with some of the common pathogens, particularly Streptococcus pneumoniae, group A streptococci, and H. influenzae. The emergence of macrolide resistance with these common pathogens may limit the clinical usefulness of this class of antimicrobial agents in the future.
Topics: Adult; Anti-Bacterial Agents; Azithromycin; Child; Clarithromycin; Drug Resistance, Microbial; Erythromycin; Humans; Microbial Sensitivity Tests
PubMed: 10377939
DOI: 10.4065/74.6.613 -
Expert Review of Anti-infective Therapy Feb 2022It is fortunate that an international panel of experts proposed definitions for multidrug-resistant (MDR) and extensively drug-resistant (XDR) in the past.
INTRODUCTION
It is fortunate that an international panel of experts proposed definitions for multidrug-resistant (MDR) and extensively drug-resistant (XDR) in the past.
AREAS COVERED
In our opinion, these definitions need amendments in order to be semantically more accurate.
EXPERT OPINION
We suggest for the MDR definition to add to 'MDR is defined as non-susceptibility to at least one agent in three or more antimicrobial categories' that this non-susceptibility is at most to the total number of all antimicrobial categories minus two, so that the definition reads: MDR is defined as non-susceptibility to at least one agent in three or more antimicrobial categories and up to (and including) the total number of all antimicrobial categories minus two. We suggest that the experts' definition of XDR as 'non-susceptibility to at least one agent in all but two or fewer antimicrobial categories (i.e. bacterial isolates remain susceptible to only one or two categories)' has to be modified regarding the content of the parenthesis to: (i.e. bacterial isolates remain susceptible to only one or two or even none antimicrobial category [in this latter setting bacterial isolates are resistant to at least one antimicrobial agent in all antimicrobial categories and concurrently there is at least one antimicrobial agent to which the isolate is susceptible to]).
Topics: Anti-Bacterial Agents; Anti-Infective Agents; Bacteria; Drug Resistance, Multiple, Bacterial; Humans; Microbial Sensitivity Tests
PubMed: 34152887
DOI: 10.1080/14787210.2021.1945922 -
Medical Hypotheses Oct 2019Infections due to resistant bacteria are the life-threatening and leading cause of mortality worldwide. The current therapy for bacterial infections includes treatment...
Infections due to resistant bacteria are the life-threatening and leading cause of mortality worldwide. The current therapy for bacterial infections includes treatment with various drugs and antibiotics. The misuse and over usage of these antibiotics leads to bacterial resistance. There are several mechanisms by which bacteria exhibit resistance to some antibiotics. These include drug inactivation or modification, elimination of antibiotics through efflux pumps, drug target alteration, and modification of metabolic pathway. However, it is difficult to treat infections caused by resistant bacteria by conventional existing therapy. In the present study binding affinities of some glitazones against ParE and MurE bacterial enzymes are investigated by in silico methods. As evident by extra-precision docking and binding free energy calculation (MM-GBSA) results, rivoglitazone exhibited higher binding affinity against both ParE and MurE enzymes compared to all other selected compounds. Further molecular dynamic (MD) simulations were performed to validate the stability of rivoglitazone/4MOT and rivoglitazone/4C13 complexes and to get insight into the binding mode of inhibitor. Thus, we hypothesize that structural modifications of the rivoglitazone scaffold can be useful for the development of an effective antibacterial agent.
Topics: Anti-Bacterial Agents; Bacterial Infections; Bacterial Proteins; DNA Topoisomerase IV; Drug Resistance, Microbial; Humans; Hydrogen Bonding; Molecular Docking Simulation; Molecular Dynamics Simulation; Peptide Synthases; Structure-Activity Relationship; Thiazolidinediones; Thiazolidines
PubMed: 31443754
DOI: 10.1016/j.mehy.2019.109305