scholarly journals Low In Vitro Antifungal Activity of Tavaborole against Yeasts and Molds from Onychomycosis

2018 ◽  
Vol 62 (12) ◽  
Author(s):  
Mahdi Abastabar ◽  
Iman Haghani ◽  
Tahereh Shokohi ◽  
Mohammad Taghi Hedayati ◽  
Seyed Reza Aghili ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Antifungal Agents ◽  
Antifungal Drug ◽  
Content Type ◽  
Fungal Isolates ◽  
Yeasts And Molds ◽  
Low Activity ◽  
In Vitro Antifungal Activity

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.

scholarly journals 7-Chloroquinolin-4-yl Arylhydrazone Derivatives: Synthesis and Antifungal Activity

2011 ◽  
Vol 11 ◽  
pp. 1489-1495 ◽  
Author(s):  
Auri R. Duval ◽  
Pedro H. Carvalho ◽  
Maieli C. Soares ◽  
Daniela P. Gouvêa ◽  
Geonir M. Siqueira ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Rational Design ◽  
Antifungal Agents ◽  
Inhibitory Concentration ◽  
First Line ◽  
Minimum Fungicidal Concentration ◽  
Starting Point ◽  
Line Drug ◽  
In Vitro Antifungal Activity

Fifteen 7-chloro-4-arylhydrazonequinolines have been evaluated for their in vitro antifungal activity against eight oral fungi:Candida albicans, C. parapsilosis, C. lipolytica, C. tropicalis, C. famata, C. glabrata, Rhodutorula mucilaginosa, andR. glutinis. Several compounds exhibited minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC) activities comparable with the first-line drug fluconazole. These results could be considered as an important starting point for the rational design of new antifungal agents.

scholarly journals In vitro Antifungal Activity of Two Tissue Conditioners Combined with Nystatin, Miconazole and Fluconazole against Candida albicans

2012 ◽  
Vol 13 (5) ◽  
pp. 695-698 ◽  
Author(s):  
Amol Pharande ◽  
Narendra Chopde ◽  
Mayur N Khade ◽  
Yogesh R Khadtare ◽  
Sanket S Shah ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Antifungal Agents ◽  
Antifungal Drugs ◽  
P Value ◽  
Intergroup Difference ◽  
Maximum Inhibition ◽  
Post Hoc ◽  
In Vitro Antifungal Activity

ABSTRACT Aim To determine and compare antifungal activity of two tissue conditioners combined with nystatin, miconazole and fluconazole against Candida albicans. Materials and methods Two tissue conditioners Viscogel and GC Soft combined with nystatin, miconazole and fluconazole were tested against Candida albicans using agar core inhibition diameter assay. One-way analysis of variance followed by Tukey's post-hoc test was used to test the intergroup difference. p-value < 0.05 was considered statistically significant. Results Maximum inhibition was seen in the fluconazole groups followed by miconazole and the least inhibition was seen in case of nystatin group. Conclusion Tissue conditioners when mixed with antifungal agents showed satisfactory inhibition of Candida albicans. Clinical significance Incorporation of antifungal drugs into tissue conditioners shows good inhibition of C. albicans and can be recommended for clinical use. How to cite this article Chopde N, Pharande A, Khade MN, Khadtare YR, Shah SS, Apratim A. In vitro Antifungal Activity of Two Tissue Conditioners Combined with Nystatin, Miconazole and Fluconazole against Candida albicans. J Contemp Dent Pract 2012;13(5):695-698.

scholarly journals In Vitro Antifungal Activity of Luliconazole, Efinaconazole, and Nine Comparators Against Aspergillus and Candida Strains Isolated from Otomycosis

2021 ◽  
Vol 14 (4) ◽  
Author(s):  
Gholamreza Shokoohi ◽  
Reza Rouhi ◽  
Mohammad Etehadnezhad ◽  
Bahram Ahmadi ◽  
Javad Javidnia ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Candida Species ◽  
Fungal Pathogens ◽  
Antifungal Agents ◽  
Geometric Mean ◽  
Antifungal Drugs ◽  
High Recurrence Rate ◽  
Broth Microdilution ◽  
In Vitro Antifungal Activity

Background: Aspergillus and Candida species are the most commonly identified fungal pathogens in otomycosis. However, we usually encounter some difficulties in its treatment because many patients show resistance to antifungal agents and present a high recurrence rate. Objectives: The current research was conducted to compare the in vitro activities of luliconazole (LUL), and efinaconazole (EFN) and the nine comparators on Aspergillus and Candida strains isolated from otomycosis. Methods: The in vitro activities of nine common antifungal drugs (amphotericin B (AMB), voriconazole (VRC), fluconazole (FLU), itraconazole (ITC), ketoconazole (KTO), clotrimazole (CLO), nystatin (NYS), terbinafine (TRB), and caspofungin (CAS)) and two novel new azoles (LUL and EFN) against of 108 clinical isolates of Aspergillus and Candida species obtained from otomycosis were assessed according to the CLSI broth microdilution document. Results: The LUL and EFN had the geometric mean minimum inhibitory concentrations (GM MICs) of 0.098 and 0.109 μg/mL against all Aspergillus strains, respectively. Furthermore, the GM MICs of all Candida isolates for LUL, EFN, CAS, CLO, VRC, AMB, ITC, KTO, FLU, NYS, and TRB were calculated to be 0.133, 0.144, 0.194, 0.219, 0.475, 0.537, 0.655, 1.277, 4.905, 9.372, and 13.592 μg/mL, respectively. Additionally, 6 (35.29%), 2 (11.7%), and 1 (5.88%) Candida isolates were resistant to FLU, CAS, and VRC, respectively. Conclusions: As the findings indicated, LUL and EFN showed the lowest GM MIC values against the examined species. Accordingly, these novel imidazole and triazole antifungal agents can be regarded as proper candidates for the treatment of otomycosis caused by Aspergillus and Candida strains.

scholarly journals Synthesis of Novel Thiazolyl Hydrazine Derivatives and Their Antifungal Activity

2021 ◽  
Vol 2021 ◽  
pp. 1-8
Author(s):  
Jianjun Zhu ◽  
Yazhen Chen ◽  
Fen Su ◽  
Peiyi Wang
Keyword(s):  
Antifungal Activity ◽  
Mycelial Growth ◽  
Antifungal Agents ◽  
Biological Assessment ◽  
Botryosphaeria Dothidea ◽  
Hydrazine Derivatives ◽  
Mycelial Growth Rate ◽  
Rate Method ◽  
In Vitro Antifungal Activity

A series of novel thiazolyl hydrazine derivatives 3a–3o were synthesized and evaluated for their in vitro antifungal activity against six phytopathogenic strains, namely, Botryosphaeria dothidea (B. d.), Gibberella sanbinetti (G. s.), Fusarium oxysporum (F. o.), Thanatephorus cucumeris (T. c.), Sclerotinia sclerotiorum (S. s.), and Verticillium dahliae (V. d.), by the classical mycelial growth rate method. Biological assessment results showed that most of these target compounds showed good antifungal activity toward tested strains. Especially, compound 3l showed excellent antifungal activities against B. d. and G. s. with relatively lower EC50 values of 0.59 and 0.69 µg/mL, respectively, which were extremely superior to those of commercial fungicides fluopyram, boscalid, and hymexazol and were comparable to those of carbendazim. Given the excellent bioactivity of designed compounds, this kind of thiazolyl hydrazine framework can provide a suitable point for exploring highly efficient antifungal agents.

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 ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Trichophyton Rubrum ◽  
Geometric Mean ◽  
Clinical Isolates ◽  
The Novel ◽  
Large Collection ◽  
Content Type ◽  
Trichophyton Interdigitale ◽  
In Vitro Antifungal Activity

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 .

scholarly journals Antifungal Susceptibility of Emerging Dimorphic Pathogens in the Family Ajellomycetaceae

2017 ◽  
Vol 62 (1) ◽  
Author(s):  
Karolina Dukik ◽  
Abdullah M. S. Al-Hatmi ◽  
Ilse Curfs-Breuker ◽  
Dirk Faro ◽  
Sybren de Hoog ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Antifungal Agents ◽  
Geometric Mean ◽  
Antifungal Susceptibility ◽  
Effective Concentration ◽  
Dimorphic Fungi ◽  
Minimum Effective Concentration ◽  
Content Type ◽  
The Family

ABSTRACT The in vitro susceptibilities of 24 molecularly identified dimorphic fungi belonging to the genera Adiaspiromyces, Blastomyces, and Emergomyces within the family Ajellomycetaceae were tested against 8 standard antifungal agents using CLSI document M38-A2. Amphotericin B and posaconazole had the lowest geometric mean MICs (<0.05 μg/ml) followed by itraconazole (<0.07 μg/ml), voriconazole (<0.15 μg/ml), and isavuconazole (<0.42 μg/ml) while fluconazole was not active. Micafungin demonstrated good in vitro antifungal activity against Emergomyces (geometric mean minimum effective concentration [GM MEC] 0.1 μg/ml) and Blastomyces (GM MEC <0.017 μg/ml).

scholarly journals In Vitro and In Vivo Assessment of FK506 Analogs as Novel Antifungal Drug Candidates

2018 ◽  
Vol 62 (11) ◽  
Author(s):  
Yeonseon Lee ◽  
Kyung-Tae Lee ◽  
Soo Jung Lee ◽  
Ji Yoon Beom ◽  
Areum Hwangbo ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Pathogenic Fungi ◽  
Antifungal Drugs ◽  
Antifungal Drug ◽  
Immunosuppressive Activity ◽  
Activated T Cells ◽  
Content Type ◽  
Antifungal Efficacy

ABSTRACT FK506 (tacrolimus) is an FDA-approved immunosuppressant indicated for the prevention of allograft rejections in patients undergoing organ transplants. In mammals, FK506 inhibits the calcineurin-nuclear factor of activated T cells (NFAT) pathway to prevent T-cell proliferation by forming a ternary complex with its binding protein, FKBP12, and calcineurin. FK506 also exerts antifungal activity by inhibiting calcineurin, which is essential for the virulence of human-pathogenic fungi. Nevertheless, FK506 cannot be used directly as an antifungal drug due to its immunosuppressive action. In this study, we analyzed the cytotoxicity, immunosuppressive activity, and antifungal activity of four FK506 analogs, 31-O-demethyl-FK506, 9-deoxo-FK506, 9-deoxo-31-O-demethyl-FK506, and 9-deoxo-prolyl-FK506, in comparison with that of FK506. The four FK506 analogs generally possessed lower cytotoxicity and immunosuppressive activity than FK506. The FK506 analogs, except for 9-deoxo-prolyl-FK506, had strong antifungal activity against Cryptococcus neoformans and Candida albicans, which are two major invasive pathogenic yeasts, due to the inhibition of the calcineurin pathway. Furthermore, the FK506 analogs, except for 9-deoxo-prolyl-FK506, had strong antifungal activity against the invasive filamentous fungus Aspergillus fumigatus. Notably, 9-deoxo-31-O-demethyl-FK506 and 31-O-demethyl-FK506 exhibited robust synergistic antifungal activity with fluconazole, similar to FK506. Considering the antifungal efficacy, cytotoxicity, immunosuppressive activity, and synergistic effect with commercial antifungal drugs, we selected 9-deoxo-31-O-demethyl-FK506 for further evaluation of its in vivo antifungal efficacy in a murine model of systemic cryptococcosis. Although 9-deoxo-31-O-demethyl-FK506 alone was not sufficient to treat the cryptococcal infection, when it was used in combination with fluconazole, it significantly extended the survival of C. neoformans-infected mice, confirming the synergistic in vivo antifungal efficacy between these two agents.

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