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

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.

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.


2011 ◽  
Vol 11 ◽  
pp. 1489-1495 ◽  
Author(s):  
Auri R. Duval ◽  
Pedro H. Carvalho ◽  
Maieli C. Soares ◽  
Daniela P. Gouvêa ◽  
Geonir M. Siqueira ◽  
...  

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.


2019 ◽  
Vol 74 (11-12) ◽  
pp. 811-818 ◽  
Author(s):  
Lingling Fan ◽  
Bilan Luo ◽  
Zhongfu Luo ◽  
Li Zhang ◽  
Judi Fan ◽  
...  

AbstractIn order to obtain novel bioactive compounds with significant antifungal activities, two series of 3-substituted phthalide derivatives were designed and synthesized via reduction, bromine substitution, and etherification. In addition, the antifungal activities of all target compounds against nine phytopathogenic fungi in vitro were tested by using the mycelial growth rate method at the concentration of 50 μg mL−1. Preliminary bioassay tests showed that some compounds exhibited more potent antifungal activities as compared with hymexazol. The preliminary structure-activity relationships (SARs) of all target compounds were also investigated.


2012 ◽  
Vol 13 (5) ◽  
pp. 695-698 ◽  
Author(s):  
Amol Pharande ◽  
Narendra Chopde ◽  
Mayur N Khade ◽  
Yogesh R Khadtare ◽  
Sanket S Shah ◽  
...  

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.


Toxins ◽  
2019 ◽  
Vol 11 (10) ◽  
pp. 579 ◽  
Author(s):  
Mariana Paiva Rodrigues ◽  
Andrea Luciana Astoreca ◽  
Águida Aparecida de Oliveira ◽  
Lauranne Alves Salvato ◽  
Gabriela Lago Biscoto ◽  
...  

Aspergillus carbonarius is a saprobic filamentous fungus, food spoiling fungus and a producer of ochratoxin A (OTA) mycotoxin. In this study, the in vitro antifungal activity of neem oil (0.12% p/p of azadirachtin) was evaluated against the growth of six strains of A. carbonarius and the production of OTA. Four different concentrations of neem oil were tested in addition to three incubation times. Only the concentration of 0.3% of neem oil inhibited more than 95% of the strain’s growth (97.6% ± 0.5%), while the use of 0.5% and 1.0% of neem oil showed lower antifungal activity, 40.2% ± 3.1 and 64.7% ± 1.1, respectively. There was a complete inhibition of OTA production with 0.1% and 0.3% neem oil in the four strains isolated in the laboratory from grapes. The present study shows that neem essential oil can be further evaluated as an auxiliary method for the reduction of mycelial growth and OTA production.


2021 ◽  
Vol 14 (4) ◽  
Author(s):  
Gholamreza Shokoohi ◽  
Reza Rouhi ◽  
Mohammad Etehadnezhad ◽  
Bahram Ahmadi ◽  
Javad Javidnia ◽  
...  

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.


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