scholarly journals In Vitro Antifungal Activity of Novel Triazole Efinaconazole and Five Comparators against Dermatophyte Isolates

2018 ◽  
Vol 62 (5) ◽  
Author(s):  
Ali Rezaei-Matehkolaei ◽  
Sadegh Khodavaisy ◽  
Mohamad Mahdi Alshahni ◽  
Takashi Tamura ◽  
Kazuo Satoh ◽  
...  

ABSTRACT The objective of this study was to assess the in vitro activity of the novel triazole antifungal drug, efinaconazole, and five comparators (luliconazole, lanoconazole, terbinafine, itraconazole, and fluconazole) against a large collection of Trichophyton interdigitale and Trichophyton rubrum clinical isolates. The geometric mean MICs were the lowest for luliconazole (0.0005 μg/ml), followed by lanoconazole (0.002 μg/ml), efinaconazole (0.007 μg/ml), terbinafine (0.011 μg/ml), itraconazole (0.095 μg/ml), and fluconazole (12.77 μg/ml). It appears that efinaconazole, lanoconazole, and luliconazole are promising candidates for the treatment of dermatophytosis due to T. interdigitale and T. rubrum .

Author(s):  
Shahram Mahmoudi ◽  
Mahmoud Vahidi ◽  
Ebadollah Shiri Malekabad ◽  
Alireza Izadi ◽  
Mehrdad Khatami ◽  
...  

Background: Dermatophytosis is a globally distributed fungal infection. Treatment failure and relapse is common in this disease. Silver nanoparticle are known for their promising antimicrobial activity. The aim of this study was to determine the antifungal activity of these nanoparticles against common dermatophyte species. Methods: A set of 30 molecularly identified dermatophytes including Trichophyton interdigitale (n=10), Trichophyton rubrum (n=10), and Epidermophyton floccosum (n=10) were used in this study. Green synthesized silver nanoparticles using chicory (Cichorium intybus) were tested for their antifungal activity in comparison to fluconazole, itraconazole and terbinafine. Interspecies differences in minimum inhibitory concentrations of antifungal drugs and silver nanoparticles were tested using Kruskal–Wallis test in SPSS software version 21. Results: The highest minimum inhibitory concentrations (MICs) among antifungal drugs were observed for fluconazole [range: 4–64 µg/mL, geometric mean (GM) =17.959 µg/mL], followed by itraconazole (range: 0.008–0.5, GM= 0.066) and terbinafine (range: 0.004– 0.25 µg/mL, GM=0.027 µg/mL). Silver nanoparticles showed potent antifungal activity against all dermatophyte isolates with MICs (range: 0.25–32 µg/mL, GM=4.812 µg/mL) higher than those of itraconazole and terbinafine, but lower than fluconazole. MIC values of silver nanoparticles demonstrated significant differences between species (P=0.044), with E. floccosum having the highest MICs (GM=9.849 µg/mL) compared to T. interdigitale (GM=3.732 µg/mL) and T. rubrum (GM=3.031 µg/mL). Conclusion: Silver nanoparticles demonstrated promising anti-dermatophyte activity against the studied dermatophytes. Due to their widespectrum activity against other fungal and bacterial pathogens, they could be a potential choice, at least in the case of cutaneous and superficial infections.


2016 ◽  
Vol 60 (4) ◽  
pp. 2528-2531 ◽  
Author(s):  
Shawn R. Lockhart ◽  
Annette W. Fothergill ◽  
Naureen Iqbal ◽  
Carol B. Bolden ◽  
Nina T. Grossman ◽  
...  

ABSTRACTThein vitroactivities of the novel fungal Cyp51 inhibitor VT-1129 were evaluated against a large panel ofCryptococcus neoformansandCryptococcus gattiiisolates. VT-1129 demonstrated potent activities against bothCryptococcusspecies as demonstrated by low MIC50and MIC90values. ForC. gattii, thein vitropotency was maintained against all genotypes. In addition, significantly lower geometric mean MICs were observed for VT-1129 than for fluconazole againstC. neoformans, including isolates with reduced fluconazole susceptibility.


2018 ◽  
Vol 62 (12) ◽  
Author(s):  
Mahdi Abastabar ◽  
Iman Haghani ◽  
Tahereh Shokohi ◽  
Mohammad Taghi Hedayati ◽  
Seyed Reza Aghili ◽  
...  

ABSTRACT The in vitro activity of tavaborole, an FDA-approved antifungal drug, was compared to that of four antifungal agents against 170 clinical fungal isolates originating from patients with onychomycosis. Tavaborole had low activity against all isolates compared to itraconazole, terbinafine, and fluconazole, the principal choices for treatment of onychomycosis. Thus, it appears that tavaborole is not a candidate for the treatment of onychomycosis due to Candida species, Aspergillus species, and dermatophytes.


2019 ◽  
Vol 63 (10) ◽  
Author(s):  
Daniela Monti ◽  
Diletta Mazzantini ◽  
Silvia Tampucci ◽  
Alessandra Vecchione ◽  
Francesco Celandroni ◽  
...  

ABSTRACT Onychomycosis is a nail fungal infection, mostly caused by dermatophytes. The treatment efficacy is impaired by difficulties of reaching effective drug levels at the site of infection; frequent relapses occur after cessation of antifungal therapy. The aim of the study was to compare two commercial products containing ciclopirox or efinaconazole for antimycotic activity and antifungal drug resistance. A study of permeation and penetration through bovine hoof membranes, as a nail model, was performed to evaluate the antimycotic activity of permeates against clinical isolates of selected fungi, and the frequency of spontaneous in vitro Trichophyton rubrum-resistant strains was assessed by broth microdilution assays. The results suggest that ciclopirox creates a depot in the nail, leading to a gradual release of the drug over time with action on both the nail plate and bed. Conversely, efinaconazole, mildly interacting with nail keratin, mainly exerts its antifungal activity in the nail bed. However, in the case of T. rubrum, the antifungal activities of the drugs in the nail plate seem comparable. Finally, efinaconazole showed a potential for induction of resistance in T. rubrum, which may limit its efficacy over time. Ciclopirox did not show any potential to induce resistance in T. rubrum and appears endowed with a more complete activity than efinaconazole in the management of onychomycosis as the nail keratin is a substrate for the growth of fungal cells, and the availability of drug in large concentration just in the nail bed may not be sufficient to guarantee the complete eradication of pathogens.


2018 ◽  
Vol 62 (8) ◽  
Author(s):  
Kimberley A. Savage ◽  
Maria del Carmen Parquet ◽  
David S. Allan ◽  
Ross J. Davidson ◽  
Bruce E. Holbein ◽  
...  

ABSTRACTCandida albicansis an important opportunistic pathogen causing various human infections that are often treated with azole antifungals. The U.S. CDC now regards developing candidal antifungal resistance as a threat, creating a need for new and more effective antifungal treatments. Iron is an essential nutrient for all living cells, and there is growing evidence that interference with iron homeostasis ofC. albicanscan improve its response to antifungals. This study was aimed at establishing whether withholding iron by currently used medical iron chelators and the novel chelator DIBI could restrict growth and also enhance the activity of azoles against clinical isolates ofC. albicans. DIBI, but not deferoxamine or deferiprone, inhibited the growth ofC. albicansat relatively low concentrationsin vitro, and this inhibition was reversed by iron addition. DIBI in combination with various azoles demonstrated stronger growth inhibition than the azoles alone and greatly prolonged the inhibition of cell multiplication. In addition, the administration of DIBI along with fluconazole (FLC) to mice inoculated with an FLC-sensitive isolate in a model of experimentalC. albicansvaginitis showed a markedly improved clearance of infection. These results suggest that iron chelation by DIBI has the potential to enhance azole efficacy for the treatment of candidiasis.


2020 ◽  
Vol 64 (11) ◽  
Author(s):  
Cecilia G. Carvalhaes ◽  
Leonard R. Duncan ◽  
Wen Wang ◽  
Helio S. Sader

ABSTRACT Contezolid, a new oxazolidinone antibacterial agent currently in development for the treatment of skin and skin structure infections, was susceptibility tested against Gram-positive clinical isolates (n = 1,211). Contezolid demonstrated potent activity against Staphylococcus aureus (MIC50/90, 0.5/1 mg/liter), coagulase-negative Staphylococcus (MIC50/90, 0.25/0.5 mg/liter), Enterococcus spp. (MIC50/90, 0.5/1 mg/liter), and streptococci (MIC50/90, 1/1 mg/liter). Moreover, methicillin-resistant S. aureus and vancomycin-resistant Enterococcus faecium isolates were all inhibited by contezolid at ≤1 mg/liter. These results support the clinical development of contezolid.


2002 ◽  
Vol 9 (1-2) ◽  
pp. 91-96 ◽  
Author(s):  
Libor Dostál ◽  
Aleš Růžička ◽  
Roman Jambor ◽  
Vladimír Buchta ◽  
Petra Kubanová ◽  
...  

The in vitro antifungal activity of compounds 1-3 ({[(CH3)2NCH2]2C6H3}R2SnX; (where X=Cl, R=n-Bu for 1, X=Br, R=n-Bu for 2 and x=PF6, R=n=Bu for 3)) was estimated with the help of a modified microdilution format of the M27-A guidelines and was compared with in vitro activity of their diphenyltin(IV) analogues 4 and 5 (where X=Br, R=Ph for 4 and X=PF6, R=Ph for 5), and of drugs currently in clinical use (ketoconazole, fluconazole and amphotericin B). It was found that in coordinating solvents the more soluble derivative 2 is less active than the phenyl one (4), and compounds 1 and 3 are even inactive.In this paper, the in vitro antitumour activity of ionic diphenyltin(IV) complexes 4 and 5 against seven tumoural cell lines of human origin is also reported. The preparation and characterization (H1, C13 and Sn119 NMR spectroscopy and electrospray ionization mass spectrometry) of the novel compound 3 is mentioned too.


2006 ◽  
Vol 12 (3) ◽  
pp. 163-165 ◽  
Author(s):  
Hiroyasu Koga ◽  
Yuri Tsuji ◽  
Kazuyoshi Inoue ◽  
Kazuo Kanai ◽  
Toshiro Majima ◽  
...  

2016 ◽  
Vol 61 (1) ◽  
Author(s):  
Hamed Fakhim ◽  
Saeed Emami ◽  
Afsane Vaezi ◽  
Seyedeh Mahdieh Hashemi ◽  
Leila Faeli ◽  
...  

ABSTRACT The in vitro activities of two novel azole compounds (aryl-1,2,4-triazol-3-ylthio analogues of fluconazole [ATTAFs]) and five comparator antifungal agents against 52 clinical Candida isolates from 5 different species were determined. The novel azole compounds had the lowest geometric mean MICs, followed by fluconazole. Moreover, combinations of these compounds with fluconazole exhibited synergistic effects against fluconazole-susceptible (22 of 23 isolates), fluconazole-susceptible dose-dependent (10 of 13 isolates), and fluconazole-resistant (1 of 16 isolates) Candida isolates.


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