• Interactions of 4-quinolone antibacterials and antibiotics with gram negative and positive bacteria. (microbiologyresearch.org)
  • Quinolones differ in chemical structure and mode of action from (beta)-lactam antibiotics. (sdrugs.com)
  • Quinolones may, therefore, be active against bacteria resistant to (beta)-lactam antibiotics. (sdrugs.com)
  • LND belongs to the novel benzoquinolizine subclass of quinolone antibiotics and is being developed as a parenteral formulation in the form of L-arginine salt. (vjim.org)
  • The molecular structure of β-lactam antibiotics can be modified either to introduce another β-lactam ring (the pharmacophore conferring bactericidal activities to these molecules), or to add other pharmacophores that modify their pharmacological properties and spectrum of action. (encyclopedia.pub)
  • Seay TM, Peretsman SJ and Dixon PS (1996) Inhibition of human transitional cell carcinoma in vitro proliferation by fluoroquinolone antibiotics. (toku-e.com)
  • This medication belongs to a class of drugs known as quinolone antibiotics and works by inhibiting the growth of bacteria. (infectweb.com)
  • The enzyme (TEM-52) selectively degraded β-lactam antibiotics but was completely inactive against tetracycline-, quinolone-, macrolide-, or aminoglycoside-structured antibacterials. (biomedcentral.com)
  • Quinolone antibiotics are generally considered to have concentration-dependent bactericidal activity and peak/MIC and AUC/MIC ratios have been identified as possible pharmacodynamic predictors of clinical and microbiological outcome as well as the development of bacterial resistance. (perfectusbiomed.com)
  • Sparkle exerts its antibacterial activity by inhibiting DNA gyrase, a bacterial topoisomerase. (sdrugs.com)
  • It has antibacterial activity against a broad spectrum of Gram negative and Gram positive bacteria (See Tables I and II). (drugs.com)
  • Some quinolone and fluoroquinolone drugs chemical structures. (hindawi.com)
  • The in vitro activities of BMS-284756 (a novel des-fluoroquinolone), levofloxacin, moxifloxacin, and clarithromycin were tested against 5 strains of Chlamydia trachomatis and 20 isolates of Chlamydia pneumoniae. (suny.edu)
  • Levonadifloxacin (LND) is a broad-spectrum benzoquinolizine fluoroquinolone with potent activity against quinolone-resistant S. aureus and MRSA phenotypes developed by an Indian company Wockhardt. (vjim.org)
  • Although culture and susceptibility data (C&S) can be a powerful tool to guide selection, it remains an in vitro test that is applied to in vivo conditions and over-reliance on the information it provides can lead to therapeutic failure. (vin.com)
  • Despite the perfectly cultured organism, C&S data is inherently deficient because the in vitro methods used do not mimic in vivo conditions. (vin.com)
  • In order to determine in vitro and in vivo the involvement of tannins and flavonoids in the anthelmintic activity of Newbouldia laevis and Zanthoxylum zanthoxyloïdes (Fagara zanthoxyloïdes) on adult worms of H. contortus, Djallonke ovine infested by H. contortus have been treated ad libitum with cool leaves of Z. zanthoxyloïdes associated or no to an inhibitor of tannins, the poly ethylene glycol (PEG) on seven consecutive days. (eujournal.org)
  • In terms of clinical, pharmacological in-vitro and in-vivo biological activities, E. arvense has a promising efficacy. (researchgate.net)
  • To test this possibility, we assessed the catalytic activity in vitro of purified TEM-52 enzymes obtained by recombinant DNA techniques, followed by an in vivo activity test in carp after administration of cefazolin, a β-lactam antibiotic. (biomedcentral.com)
  • In vitro susceptibility testing and molecular resistance testing may be useful to guide therapy, especially for disseminated infections if available. (medscape.com)
  • Also, often it is difficult to compare in vitro susceptibility results with data reported by other investigators because of differences in methodology, e.g., lack of interlaboratory standardization of inocula (e.g.,104 versus102 CFU/ml), and use of a broth microdilution method versus agar dilution or disk diffusion methods. (antimicrobe.org)
  • Correcting the limited aqueous solubility and the high susceptibility to cyt b Qo site resistant parasites found in the clinic will be major obstacles in the future development of the 3-oxadiazole quinolone antimalarial class I. (tcgls.com)
  • Ofloxacin is commonly used in clinical in vitro microbiological antimicrobial susceptibility tests (panels, discs, and MIC strips) against Gram-positive and Gram-negative microbial isolates. (toku-e.com)
  • Another hypothesis supports the existence of a cooperative bond between the quinolone-DNA-DNA-gyrase [ 8 - 11 ]. (hindawi.com)
  • Quinolone carboxylic acid derivatives are classified as DNA gyrase inhibitors. (drugs.com)
  • It was developed by Daiichi Seiyaku to be resistant to metabolic oxidation in the liver and inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication. (toku-e.com)
  • Sparfloxacin inhibits the supercoiling activity of DNA gyrase which is an enzyme essential for DNA replication thus promoting the breakage of DNA structures. (ekbd.net)
  • While tetracyclines, macrolides, lincosamides, and quinolones have historically been used for treatment of infections due to these organisms, acquired resistance is now well documented and varies according to drug, organism, and patient population. (medscape.com)
  • Since Lescher and col. prepared the nalidixic acid in 1962 [ 1 ], the synthesis of new quinolones continues (Figure 1 ). (hindawi.com)
  • Quinolones inhibit the bacterial DNA synthesis [ 2 ], and there are several hypotheses to explain their mechanism of action. (hindawi.com)
  • In the present work we reported the synthesis, characterization, and biological activity results of a copper mixed complex (see Figure 1 ), with hsm and nalidixic acid. (hindawi.com)
  • The interesting activities of a subset of 4-hydoxy-2-pyridones provided the impetus for synthesis of additional chemotypes with this core ( Figure 1 ) and their evaluation for effectiveness against additional pathogenic strains including Ng and N. meningitidis (Nm ). (elifesciences.org)
  • The bactericidal activity of Oxacillin results from the inhibition of cell wall synthesis and is mediated through Oxacillin binding to penicillin binding proteins (PBPs). (ncats.io)
  • Ofloxacin inhibited proliferation and DNA synthesis of these 3 human TCC lines (CCSUP, T24, and J82 ) in vitro . (toku-e.com)
  • In order to elucidate the first step of the 4-quinolone synthesis pathway in P. aeruginosa, we have characterized the function of the pqsA gene product. (ecu.edu)
  • The described 2-pyrazoyl series displays improved DMPK properties, including improved aqueous solubility compared to previously reported quinolone series and acceptable safety margin through in vitro cytotoxicity assessment. (liverpool.ac.uk)
  • The optimized analog compound I (R = 4-methylpiperidin-1-yl) showed robust metabolic stability in vitro, although the aqueous solubility was limited. (tcgls.com)
  • The cephalosporin class of antimicrobial agents is known for its broad spectrum of activity, proven efficiency and favorable safety profile, making it the most commonly prescribed class of antimicrobials. (biomedcentral.com)
  • Evo 500 mg/100 ml is contraindicated in patients with a history of hypersensitivity to Evo 500 mg/100 ml and other quinolone antimicrobial agents or any other components of this product. (medeasy.health)
  • We identified two novel orally active inhibitors, PTC-847 and PTC-672, that exhibit a narrow spectrum of activity against Ng including MDR isolates. (elifesciences.org)
  • Cadi, R. dc.description.abstract: Background: The success of in vitro-fertilization (IVF) cycles is determined in large part by the quality of embryo cleavage, which in turn, is dependent on the quality of the embryo culture media (CM). Many factors can influence the quality of embryo CM, one of which is the levels of Cell Free Deoxyribonucleic acid (DNA). (who.int)
  • A series of 2-pyrazolyl quinolones has been designed and synthesized in 5-7 steps to optimize for both in vitro antimalarial potency and various in vitro drug metabolism and pharmacokinetics (DMPK) features. (liverpool.ac.uk)
  • To discover new antimalarial chemotypes, we screened the Janssen Jumpstarter library against the P. falciparum asexual parasite and identified the 7-N-substituted-3-oxadiazole quinolone hit class I [R = pyrrolidin-1-yl, 4-acetylpiperazin-1-yl, azepan-1-yl, etc. (tcgls.com)
  • We established the structure-activity relationship and optimized the antimalarial potency. (tcgls.com)
  • In order to address these deficiencies, a series of quinolones based novel molecules have been synthesized and evaluated as potential antitrypanosomal agents. (unibas.ch)
  • Biochemical, biophysical, and biological data support the efficacy of these molecules both in vitro and in mouse models. (elifesciences.org)
  • The present work constitutes a review of the literature of plants and chemically defined molecules from natural sources with in vitro anti-hypertensive potential based on the inhibition of ACE. (scielo.br)
  • The inhibitory activity on 120 isolates of seven canine urinary pathogens was also investigated and is listed in Table II. (drugs.com)
  • Additional prospective clinical research is needed to characterize quinolone pharmacodynamic parameters and answer unresolved questions regarding optimal pharmacodynamic outcome predictors for Gram-positive bacteria, anaerobes and atypical respiratory pathogens. (perfectusbiomed.com)
  • First, the antimicrobial activities of LVFX, KRM, and CAM against intracellular organisms of MTB Kurono and MAC N-444 strains were examined under conditions in which infected MM6-M phi s and A-549 cells were cultured for up to 7 days or longer in medium containing the antimicrobials at their Cmaxs in the blood, achievable after oral administration of clinical dosages of these drugs. (nih.gov)
  • Since these organisms require highly specialized conditions for culture in vitro and because molecular-based detection is not widely available (except for M genitalium), clinicians must be aware of the clinical syndromes with which these organisms have been associated and have a high level of suspicion prompting them to order the appropriate diagnostic tests from reference laboratories. (medscape.com)
  • In vitro activities of BMS-284756 against Chlamydia trachomatis and recent clinical isolates of Chlamydia pneumoniae. (suny.edu)
  • Malay S, Roblin PM, Reznik T, Kutlin A, Hammerschlag MR. In vitro activities of BMS-284756 against Chlamydia trachomatis and recent clinical isolates of Chlamydia pneumoniae. (suny.edu)
  • In vitro activity of garenoxacin against recent clinical isolates of Chlamydia pneumoniae. (suny.edu)
  • In vitro activities of gemifloxacin (SB 265805, LB20304) against recent clinical isolates of Chlamydia pneumoniae. (suny.edu)
  • The MIC values for enrofloxacin against these isolates are presented in Table I. Most strains of these organisms were found to be susceptible to enrofloxacin in vitro but the clinical significance has not been determined for some of the isolates. (drugs.com)
  • The 2-pyrazolyl quinolones are believed to bind to the ubiquinone-reducing Qi site of the parasite bc1 complex, which is supported by crystallographic studies of bovine cytochrome bc1 complex. (liverpool.ac.uk)
  • Fleroxacin is a quinolone antibiotic. (wikipedia.org)
  • In vitro activity of nemonoxacin, a novel nonfluorinated quinolone antibiotic, against Chlamydia trachomatis and Chlamydia pneumoniae. (suny.edu)
  • Levofla is a bacterial medication or antibiotic that exhibits a bacteriostatic activity, they act by inhibiting the growth of bacteria. (arvidweb.com)
  • The antimicrobial effects of LVFX and KRM against respectively MTB and MAC within A-549 cells were significantly less than the activities they displayed against the same organisms residing in MM6-M phi s. (nih.gov)
  • National Guard Hospital in Jeddah or Qatif activity against Gram-positive organisms, Central Hospital in Qatif. (who.int)
  • In-vitro metabolic inhibition studies using rat and human liver microsomes and intestinal absorption studies of riluzole in a rat everted gut-sac model were conducted to elucidate the mechanism of interaction. (researchgate.net)
  • In vitro studies using liver microsomes show that hydroxylation of the primary amine group producing N-hydroxyriluzole is the main metabolic pathway in human, monkey, dog and rabbit. (nih.gov)
  • The Pseudomonas quinolone signal (PQS) is a 3-hydroxy-4-quinolone with a 2-alkyl substitution which is synthesized by the condensation of anthranilic acid with a 3-keto-fatty acid. (ecu.edu)
  • Fourth generation quinolones include the trovofloxacin with an effectiveness against anaerobic organism [ 4 ]. (hindawi.com)
  • Oxacillin has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria. (ncats.io)
  • For example, to date, hundreds of cephalosporin derivatives are available and they are classified into five "generations" that are characterized by different ways of administration and by an enhanced microbicidal activity towards Gram-negative bacteria (while the founder molecule is mainly active on Gram-positive bacteria) [ 12 ] . (encyclopedia.pub)
  • Enrofloxacin is a synthetic chemotherapeutic agent from the class of the quinolone carboxylic acid derivatives. (drugs.com)
  • Degradation activity of TEM-52 against various classes of antimicrobials was assessed incubating the β-lactamase enzyme solution (25 mU/ml) with various antimicrobials. (biomedcentral.com)
  • Fleroxacin is contraindicated in patients with a history of hypersensitivity to the substance or any other member of the quinolone class, or any component of the medicine. (wikipedia.org)
  • In vitro studies predict that CYP 2D6, CYP 2C19, CYP 3A4 and CYP 2E1 are unlikely to contribute significantly to riluzole metabolism in humans. (nih.gov)
  • Fleroxacin and other fluoroquinolones, are known to trigger seizures or lower the seizure threshold, due to their inhibitory activity on GABA receptor binding. (wikipedia.org)
  • In-vitro activity of gatifloxacin against Chlamydia trachomatis and Chlamydia pneumoniae. (suny.edu)
  • BMS-284756 was the most active quinolone tested. (suny.edu)
  • Some metabolites appear pharmacologically active in in vitro assays. (nih.gov)
  • Sterile dressings may also be a glycoprotein produced by almost all activities consisting of an active substance. (stonecottagegardens.com)
  • In comparison to quercetin and ascorbic acid, the scavenging of superoxide radical (SOR), hydrogen peroxide, and 2, 2-Diphenyl-2-picrylhydrazyl (DPPH) radical activity by a model (most biologically active) of the anticancer plant was also evaluated. (who.int)
  • The successful identification of meaningful pharmacodynamic outcome parameters can, therefore, greatly assist clinicians in making objective prescribing decisions rather than relying on static in vitro MIC data. (perfectusbiomed.com)
  • There is considerable variation in pharmacodynamic calculations and outcome parameters appear to be quinolone- and pathogen-specific. (perfectusbiomed.com)
  • Furthermore, members of the series retain moderate activity against the atovaquone-resistant parasite isolate (TM90C2B). (liverpool.ac.uk)
  • Clearly, in vitro methods can not take into account host factors which detract from efficacy. (vin.com)
  • The effect may be related to impairment of telomerase activity by some unknown mechanism (Yamakuchi M et al, 1997). (toku-e.com)
  • Sparkle has in vitro activity against a wide range of gram-negative and gram-positive microorganisms. (sdrugs.com)
  • Against gram-negative bacilli, the in vitro activity of BLFX was the same or slightly lower than that of the other drugs. (elsevierpure.com)
  • In in vitro tests, riluzole protected cultured rat motor neurons from the excitotoxic effects of glutamic acid and prevented the death of cortical neurons induced by anoxia. (nih.gov)
  • There is marked interindividual variability in the clearance of riluzole, probably attributable to variability of CYP 1A2 activity, the principal isozyme involved in N-hydroxylation. (nih.gov)
  • Several pharmacological activities of E. arvense such as anticancer, anti-inflammatory, antibacterial, antifungal and antidiabetics support its traditional uses. (researchgate.net)
  • The present study was designed to evaluate the analgesic and anti-inflammatory activity of "Trichilia connaroides" bark using different animal models. (asianjpr.com)
  • Anti-inflammatory activity was evaluated using Formalin induced paw edema model, Croton oil ear edema in rats. (asianjpr.com)
  • Evaluation of anti inflammatory activity was done by Formalin induced paw edema model, Croton oil ear edema model. (asianjpr.com)
  • The study revealed that the "Trichilia connaroides"bark possess a significant analgesic and anti-inflammatory activity. (asianjpr.com)
  • D, Narayana Swamy V.B. Pharmacological Evaluation of Trichilia connaroides Bark for Analgesic and Anti-inflammatory activity in Experimental Animal Models. (asianjpr.com)
  • Effects of Anti-Inflammatory Activity of Mimosa pudica. (asianjpr.com)
  • These results indicate that the PqsA protein is responsible for priming anthranilate for entry into the PQS biosynthetic pathway and that this enzyme may serve as a useful in vitro indicator for potential agents to disrupt quinolone signaling in P. aeruginosa. (ecu.edu)
  • The TEM-52 enzyme was eluted in 20 mM Tris buffer (pH 7.0) and adjusted to contain 500 mU/ml β-lactamase activity when assayed for 5 min using nitrocefin (50 μg/ml, Oxoid, Basingstoke, UK) as the substrate (O'Callaghan et al. (biomedcentral.com)