scholarly journals High in vitro activity of a novel dual bacterial topoisomerase inhibitor of the ATPase activities of GyrB and ParE (VT12-008911) against Neisseria gonorrhoeae isolates with various high-level antimicrobial resistance and multidrug resistance

2014 ◽  
Vol 69 (7) ◽  
pp. 1866-1872 ◽  
Author(s):  
S. Jeverica ◽  
D. Golparian ◽  
B. Hanzelka ◽  
A. J. Fowlie ◽  
M. Mati i  ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Antimicrobial Resistance ◽  
Neisseria Gonorrhoeae ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Topoisomerase Inhibitor ◽  
High Level

scholarly journals In Vitro Susceptibilities of 400 Spanish Isolates ofNeisseria gonorrhoeae to Gemifloxacin and 11 Other Antimicrobial Agents

2000 ◽  
Vol 44 (9) ◽  
pp. 2543-2544 ◽  
Author(s):  
S. Berrón ◽  
J. A. Vázquez ◽  
M. J. Giménez ◽  
L. de la Fuente ◽  
L. Aguilar
Keyword(s):  
Neisseria Gonorrhoeae ◽  
Antimicrobial Agents ◽  
Vitro Activity ◽  
Penicillin Resistance ◽  
In Vitro Activity ◽  
Ofneisseria Gonorrhoeae ◽  
High Level

ABSTRACT The in vitro activity of gemifloxacin versus those of 11 other antimicrobial agents against 400 strains of Neisseria gonorrhoeae was determined by microdilution with supplemented GC agar. A total of 37.5% of the strains were β-lactamase positive. A total of 70 and 6.4% of the β-lactamase-negative strains exhibited intermediate and high-level penicillin resistance, respectively. Ceftriaxone and gemifloxacin were the most active drugs (MICs at which 90% of isolates are inhibited, 0.01 versus 0.007 μg/ml, respectively), with 100% of strains inhibited by 0.12 μg/ml.

scholarly journals High in vitro activity of DIS-73285, a novel antimicrobial with a new mechanism of action, against MDR and XDR Neisseria gonorrhoeae

2020 ◽  
Vol 75 (11) ◽  
pp. 3244-3247
Author(s):  
Susanne Jacobsson ◽  
Clive Mason ◽  
Nawaz Khan ◽  
Paul Meo ◽  
Magnus Unemo
Keyword(s):  
Neisseria Gonorrhoeae ◽  
Small Molecule ◽  
Mechanism Of Action ◽  
Vitro Activity ◽  
In Vivo Studies ◽  
In Vitro Activity ◽  
Agar Dilution ◽  
High Level

Abstract Background The rising incidence of antimicrobial resistance in Neisseria gonorrhoeae may result in untreatable gonorrhoea in certain circumstances and development of novel antimicrobials is urgently needed. Objectives To evaluate the in vitro activity of a novel small-molecule antimicrobial with a new mechanism of action, DIS-73285, against a large geographically, temporally and genetically diverse collection of clinical N. gonorrhoeae isolates and reference strains, including various types of high-level resistant, MDR and XDR gonococcal isolates (n = 262). Methods MICs (mg/L) of DIS-73285 were determined by agar dilution and by Etest for ceftriaxone, cefixime, azithromycin, ciprofloxacin, ampicillin, spectinomycin and tetracycline. Results DIS-73285 was substantially more potent than any of the currently or previously used therapeutic antimicrobials, with MICs ranging from ≤0.001 to 0.004 mg/L, and the MIC50, MIC90 and modal MIC all ≤0.001 mg/L (lowest MIC tested). No correlation with the MICs of DIS-73285 and the MICs of any of the currently or previously used antimicrobials was observed. Conclusions The novel chemotype, small-molecule antimicrobial DIS-73285, demonstrated high in vitro potency against all tested N. gonorrhoeae isolates. Further in vitro and in vivo studies, evaluating efficacy, resistance emergence, pharmacokinetic/pharmacodynamic parameters, toxicity and safety, should be conducted to evaluate DIS-73285 as a therapy specifically for urogenital and extra-genital gonorrhoea.

scholarly journals In vitro activity of the novel triazaacenaphthylene gepotidacin (GSK2140944) against MDR Neisseria gonorrhoeae

2018 ◽  
Vol 73 (8) ◽  
pp. 2072-2077 ◽  
Author(s):  
Susanne Jacobsson ◽  
Daniel Golparian ◽  
Nicole Scangarella-Oman ◽  
Magnus Unemo
Keyword(s):  
Antimicrobial Resistance ◽  
Neisseria Gonorrhoeae ◽  
Efflux Pump ◽  
Resistance Mutation ◽  
Vitro Activity ◽  
Fluoroquinolone Resistance ◽  
Cross Resistance ◽  
In Vitro Activity ◽  
The Impact

Abstract Objectives Increased antimicrobial resistance surveillance and new effective antimicrobials are crucial to maintain treatable gonorrhoea. We examined the in vitro activity of gepotidacin, a novel triazaacenaphthylene, and the effect of efflux pump inactivation on clinical Neisseria gonorrhoeae isolates and international reference strains (n = 252) and compared gepotidacin with antimicrobials currently or previously recommended for gonorrhoea treatment. Methods MICs (mg/L) were determined by agar dilution (gepotidacin) or by Etest (seven other antimicrobials). The gyrA and parC genes were sequenced and the impact of inactivation of the MtrCDE, MacAB and NorM efflux pumps on gepotidacin MICs was examined. Results Gepotidacin showed potent in vitro activity against all gonococcal isolates (n = 252; MIC ≤4 mg/L). The modal MIC, MIC50, MIC90 and MIC range of gepotidacin were 0.5, 0.5, 1 and 0.032–4 mg/L, respectively. Inactivation of the MtrCDE efflux pump, but not MacAB or NorM, decreased the gepotidacin MICs for most strains. No significant cross-resistance between gepotidacin and any other antimicrobials, including the fluoroquinolone ciprofloxacin, was identified. However, the ParC D86N mutation (possibly together with additional antimicrobial resistance mutation), which is associated with fluoroquinolone resistance, was associated with increased gepotidacin MICs. Conclusions Gepotidacin demonstrated high in vitro activity against gonococcal strains, indicating that gepotidacin could potentially be an effective option for gonorrhoea treatment, particularly in a dual antimicrobial therapy regimen and for patients with resistance or allergy to extended-spectrum cephalosporins. Nevertheless, elucidating in vitro and in vivo resistance emergence and mechanisms in detail, together with further gonorrhoea clinical studies, ideally also including chlamydia and Mycoplasma genitalium are essential.

scholarly journals In vitro activity of 14 antimicrobial agents against Neisseria gonorrhoeae from Spain.

1987 ◽  
Vol 63 (3) ◽  
pp. 215-216
Author(s):  
M C Lozano ◽  
J C Palomares ◽  
R Prados ◽  
E J Perea
Keyword(s):  
Neisseria Gonorrhoeae ◽  
Antimicrobial Agents ◽  
Vitro Activity ◽  
In Vitro Activity

scholarly journals Differential in vitro activity of the DNA topoisomerase inhibitor idarubicin against Trypanosoma rangeli and Trypanosoma cruzi

2012 ◽  
Vol 107 (7) ◽  
pp. 946-950 ◽  
Author(s):  
Momodou Jobe ◽  
Charles Anwuzia-Iwegbu ◽  
Ama Banful ◽  
Emma Bosier ◽  
Mubeen Iqbal ◽  
...  
Keyword(s):  
Trypanosoma Cruzi ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Trypanosoma Rangeli ◽  
Dna Topoisomerase ◽  
Topoisomerase Inhibitor

scholarly journals In Vitro Activity of the New Ketolide HMR3647 in Comparison with Those of Macrolides and Pristinamycins againstEnterococcus spp.

1998 ◽  
Vol 42 (12) ◽  
pp. 3279-3281 ◽  
Author(s):  
C. Torres ◽  
M. Zarazaga ◽  
C. Tenorio ◽  
A. Portillo ◽  
Y. Saenz ◽  
...  
Keyword(s):  
Vitro Activity ◽  
In Vitro Activity ◽  
Excellent Activity ◽  
High Level

Ninety-four erythromycin-susceptible and 107 erythromycin-resistant enterococcal strains (MIC of ≥512 μg/ml) were inhibited by the ketolide HMR3647 at MICs of ≤0.007 to 0.06 and 0.03 to 8 μg/ml, respectively. Eighteen vanA-positive isolates and 29 high-level-penicillin-resistant isolates, all of them erythromycin resistant, were inhibited by HMR3647 at an MIC range of 0.015 to 4 μg/ml. The new ketolide has excellent activity againstEnterococcus species.

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