scholarly journals Potent trifluoromethoxy, trifluoromethylsulfonyl, trifluoromethylthio and pentafluorosulfanyl containing (1,3,4-oxadiazol-2-yl)benzamides against drug-resistant Gram-positive bacteria

2020 ◽  
Vol 11 (1) ◽  
pp. 102-110
Author(s):  
George A. Naclerio ◽  
Nader S. Abutaleb ◽  
Kenneth I. Onyedibe ◽  
Mohamed N. Seleem ◽  
Herman O. Sintim
Keyword(s):  
Drug Resistant ◽  
Gram Positive ◽  
Methicillin Resistant ◽  
Gram Positive Bacteria

Switching from bacteriostatic against methicillin-resistant S. aureus to bactericidal via SCF3 or SF5 substitution.

DNA Binding Ligands with Excellent Antibiotic Potency Against Drug-Resistant Gram-Positive Bacteria.

ChemInform ◽  
2003 ◽  
Vol 34 (6) ◽  
Author(s):  
Roland W. Buerli ◽  
Yigong Ge ◽  
Sarah White ◽  
Eldon E. Baird ◽  
Sofia M. Touami ◽  
...  
Keyword(s):  
Dna Binding ◽  
Drug Resistant ◽  
Gram Positive ◽  
Gram Positive Bacteria

scholarly journals In Vitro and In Vivo Activities of DA-7867, a New Oxazolidinone, against Aerobic Gram-Positive Bacteria

2005 ◽  
Vol 49 (6) ◽  
pp. 2498-2500 ◽  
Author(s):  
Eun Jeong Yoon ◽  
Yeong Woo Jo ◽  
Sung Hak Choi ◽  
Tae Ho Lee ◽  
Jae Keol Rhee ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Streptococcus Pneumoniae ◽  
Gram Positive ◽  
Methicillin Resistant ◽  
Gram Positive Bacteria ◽  
Vancomycin Resistant Enterococci ◽  
Infection Models ◽  
Vancomycin Resistant

ABSTRACT In vitro and in vivo activities of DA-7867 were assessed against methicillin-resistant Staphylococcus aureus, vancomycin-resistant enterococci, and penicillin-resistant Streptococcus pneumoniae. All isolates were inhibited by DA-7867 at ≤0.78 μg/ml, a four-times-lower concentration than that of inhibition by linezolid. For murine infection models, DA-7867 also exhibited greater efficacy than linezolid against all isolates tested.

Activity of Oritavancin Against Gram-positive Pathogens Causing Bloodstream Infections in the United States Over 10 Years: Focus on Drug-Resistant Enterococcal Subsets (2010-2019)

2021 ◽  
Author(s):  
Cecilia G. Carvalhaes ◽  
Helio S. Sader ◽  
Jennifer M. Streit ◽  
Mariana Castanheira ◽  
Rodrigo E. Mendes
Keyword(s):  
United States ◽  
Staphylococcus Aureus ◽  
Enterococcus Faecium ◽  
Bloodstream Infections ◽  
The United States ◽  
Drug Resistant ◽  
Gram Positive ◽  
Methicillin Resistant ◽  
Vancomycin Resistant ◽  
Over Time

Oritavancin displayed potent and stable activity (MIC 90 range, 0.06-0.5 mg/L) over time (2010-2019) against Gram-positive pathogens causing bloodstream infections, including methicillin-resistant Staphylococcus aureus and resistant subsets of Enterococcus spp. Daptomycin and linezolid were also active against methicillin-resistant S. aureus and vancomycin-resistant Enterococcus . Only oritavancin and linezolid remained active against Enterococcus faecium isolates displaying an elevated daptomycin MIC (i.e., 2-4 mg/L). Proportions of methicillin-resistant S. aureus and vancomycin-resistant Enterococcus within the respective S. aureus and enterococcal populations decreased over this period.

scholarly journals Activities of Oxadiazole Antibacterials against Staphylococcus aureus and Other Gram-Positive Bacteria

2018 ◽  
Vol 62 (8) ◽  
Author(s):  
Sara Ceballos ◽  
Choon Kim ◽  
Derong Ding ◽  
Shahriar Mobashery ◽  
Mayland Chang ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Gram Positive ◽  
Methicillin Resistant ◽  
Content Type ◽  
Gram Positive Bacteria ◽  
Vancomycin Resistant Enterococci ◽  
Vancomycin Resistant ◽  
Mrsa Strains

ABSTRACT The activities of four oxadiazoles were investigated with 210 methicillin-resistant Staphylococcus aureus (MRSA) strains. MIC50 and MIC90 values of 1 to 2 and 4 μg/ml, respectively, were observed. We also evaluated the activity of oxadiazole ND-421 against other staphylococci and enterococci and in the presence of oxacillin for selected MRSA strains. The MIC for ND-421 is lowered severalfold in combination with oxacillin, as they synergize. The MIC90 of ND-421 against vancomycin-resistant enterococci is ≤1 μg/ml.

Efficacy and Safety of Linezolid in Immunocompromised Patients with Hematological Malignancy

Blood ◽  
2012 ◽  
Vol 120 (21) ◽  
pp. 4838-4838
Author(s):  
Shenxian Qian ◽  
Hua Song ◽  
Xuejin Zhang ◽  
Xuejin Zhang ◽  
Xiaohong Zhang ◽  
...  
Keyword(s):  
Hematological Malignancy ◽  
Lymphoblastic Leukemia ◽  
Adverse Event Rate ◽  
Base Number ◽  
Immunocompromised Patients ◽  
Gram Positive ◽  
Platelet Recovery ◽  
Methicillin Resistant ◽  
Gram Positive Bacteria ◽  
Linezolid Therapy

Abstract Abstract 4838 BACKGROUND: The aim of this study was to determine the safety, tolerance and efficacy of linezolid for the treatment of infections from Gram-positive bacteria in immunocompromised patients with Hematological Malignancy. METHODS: This was a prospective non-comparative unblinded and multi-center study in the Hematology Unit over a one-year period, administering combined use of linezolid in patients with Hematological Malignancy. RESULTS: Fifth-four adult patients received linezolid (600 mg, iv, q12h per day). Thirty-four children received linezolid (30 mg/kgr: 3 i.v. per day).Mean duration of linezolid administration was 12.8 days (range, 10–23days). Among the evaluable patients, fifty four were adults, the median age was 67(range, 30–101years); thirty four were children (range, 11 months-12.6 years), while the median age was 6 years. Primary diagnosis was acute lymphoblastic leukemia (forty-five patients), lymphoma (twenty-three patients), multiple myeloma (eleven patients), Aplastic anemia(four patients), myelodysplasia syndrome(one patients), leucopenia and hemophagocytic syndrome (two patient each). All patients were immunocompromised, 90% of them in the midst of chemotherapy cycles. The mean base number of platelet was 41×109/L(range, 30 – 138×109/L), platelet count less than 30×109/L patients were 28 cases (33%), among them, less than 10×109/L were 13 cases (14.8%). 27 out of 88 patients had positive blood cultures, methicillin-resistant Staphylococcus aureus, eighteen patients; Enterococcus, seven patients; Methicillin Resistant Staphylococcus Epidermidis and hemolytic streptococcus (one patient each).All patients were considered clinically cured after the end of the linezolid regimen (100% efficacy). The main adverse events were thrombocytopenia. There were 11 cases happened transient thrombocytopenia, Among them, four cases were happened within 4 days, seven cases happened four to seven days after received linezolid. Eliminate the possibility caused by reasons such as severe infection which can also result in thrombocytopenia, Linezolid related thrombocytopenia were only two cases (2.3%). Chemotherapy-induced myelotoxicity (90% patients) was not worsened during linezolid therapy. The platelet recovery time was also not lengthened during linezolid therapy. No bleeding episodes were presented, no Self-limited diarrhea were happened. The total adverse event rate was 2.3%; however, there was no premature cessation of linezolid in any patient. CONCLUSIONS: Linezolid may be another effective and safe therapy to treat infections from resistant Gram-positive bacteria in immunocompromised patients, even in children. Disclosures: No relevant conflicts of interest to declare.

DNA binding ligands targeting drug-resistant Gram-positive bacteria. Part 1: Internal benzimidazole derivatives

2004 ◽  
Vol 14 (5) ◽  
pp. 1253-1257 ◽  
Author(s):  
Roland W. Bürli ◽  
Dustin McMinn ◽  
Jacob A. Kaizerman ◽  
Wenhao Hu ◽  
Yigong Ge ◽  
...  
Keyword(s):  
Dna Binding ◽  
Benzimidazole Derivatives ◽  
Drug Resistant ◽  
Gram Positive ◽  
Gram Positive Bacteria

scholarly journals In Vitro Activities of ME1036 (CP5609), a Novel Parenteral Carbapenem, against Methicillin-Resistant Staphylococci

2004 ◽  
Vol 48 (8) ◽  
pp. 2831-2837 ◽  
Author(s):  
Mizuyo Kurazono ◽  
Takashi Ida ◽  
Keiko Yamada ◽  
Yoko Hirai ◽  
Takahisa Maruyama ◽  
...  
Keyword(s):  
Multiple Drug ◽  
Gram Negative Bacteria ◽  
Coagulase Negative Staphylococci ◽  
Gram Positive ◽  
Gram Negative ◽  
Methicillin Resistant ◽  
Gram Positive Bacteria ◽  
Multiple Drug Resistant ◽  
Time Kill

ABSTRACT ME1036, formerly CP5609, is a novel parenteral carbapenem with a 7-acylated imidazo[5,1-b]thiazole-2-yl group directly attached to the carbapenem moiety of the C-2 position. The present study evaluated the in vitro activities of ME1036 against clinical isolates of gram-positive and gram-negative bacteria. ME1036 displayed broad activity against aerobic gram-positive and gram-negative bacteria. Unlike other marketed β-lactam antibiotics, ME1036 maintained excellent activity against multiple-drug-resistant gram-positive bacteria, such as methicillin-resistant staphylococci and penicillin-resistant Streptococcus pneumoniae (PRSP). The MICs of this compound at which 90% of isolates were inhibited were 2 μg/ml for methicillin-resistant Staphylococcus aureus (MRSA), 2 μg/ml for methicillin-resistant coagulase-negative staphylococci, and 0.031 μg/ml for PRSP. In time-kill studies with six strains of MRSA, ME1036 at four times the MIC caused a time-dependent decrease in the numbers of viable MRSA cells. The activity of ME1036 against MRSA is related to its high affinity for penicillin-binding protein 2a, for which the 50% inhibitory concentration of ME1036 was approximately 300-fold lower than that of imipenem. In conclusion, ME1036 demonstrated a broad antibacterial spectrum and high levels of activity in vitro against staphylococci, including β-lactam-resistant strains.

scholarly journals A3, a Scorpion Venom Derived Peptide Analogue with Potent Antimicrobial and Antibiofilm Activity against Clinical Isolates of Multi-Drug Resistant Gram Positive Bacteria

2018 ◽  
Author(s):  
Ammar Almaaytah ◽  
Ahmad Farajallah ◽  
Ahmad Abualhaijaa ◽  
Qosay Al-balas
Keyword(s):  
Host Defense ◽  
Mammalian Cells ◽  
Scorpion Venom ◽  
Clinical Isolates ◽  
Drug Resistant ◽  
Gram Positive ◽  
Peptide Analogue ◽  
Gram Positive Bacteria ◽  
Conventional Antibiotics

Current research in the field of antimicrobials is focused on the development of novel antibiotics and antimicrobial agents to counteract the huge dilemma that the human population is mainly facing in regards to the rise of bacterial resistance and biofilm infections. Host Defense peptides (HDPs) are a promising group of molecules for antimicrobial development as they share unique characteristics suitable for antimicrobial activity including their broad spectrum of activity and potency against bacteria. AamAP1 is a novel HDP that was identified through molecular cloning from the venom of the North African scorpion Androctonus amoeruxi. In vitro antimicrobial assays revealed that the peptide displays moderate activity against different strains of Gram-positive and Gram-negative bacteria. Additionally, the peptide proved to be highly hemolytic and displaying significantly high toxicity against mammalian cells. In our study, a novel synthetic peptide analogue named A3 was designed from the naturally occurring scorpion venom host defense peptide. The design strategy depended on modifying the amino acid sequence of the parent peptide in order to increase its net positive charge, percentage helicity and optimize other physico-chemical parameters involved theoretically in HDPs activity. Accordingly, A3 was evaluated for its in vitro antimicrobial and anti-biofilm activity individually and in combination with four different types of conventional antibiotics against clinical isolates of multi-drug resistant (MDR) Gram-positive bacteria. A3 was also evaluated for its cytotoxicity against mammalian cells. A3 displayed potent and selective in vitro antimicrobial activities against a wide range of MDR Gram-positive bacteria. Our results also showed that combining A3 with conventional antibiotics displayed a synergistic mode of action which resulted in decreasing the MIC value for A3 peptide as low as 0.125 µM. These effective concentrations were associated with negligible toxicities on mammalian cells. In conclusion, A3 exhibits enhanced activity and selectivity when compared with the parent natural scorpion venom peptide. The combination of A3 with conventional antibiotics may be pursued as a potential novel treatment strategy against MDR and biofilm forming bacteria.

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