Novel pyrrolidine-2,4-dione derivatives containing pharmacophores of both hydrazine and diphenyl ether as potential antifungal agents: design, synthesis, biological evaluation, and 3D-QSAR study

2020 ◽  
Vol 44 (46) ◽  
pp. 20071-20082
Author(s):  
Hao-Ran Hu ◽  
An Wang ◽  
Ling-Ling Qiu ◽  
Xiao-Bin Wang ◽  
Min Chen ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Scanning Electron Microscopy ◽  
Antifungal Activity ◽  
Antifungal Agents ◽  
Diphenyl Ether ◽  
3D Qsar ◽  
Biological Evaluation ◽  
Qsar Study ◽  
Design Synthesis ◽  
Scanning Electron

Novel pyrrolidine-2,4-dione derivatives were designed based on natural products. Some synthesized compounds showed excellent antifungal activity. Scanning electron microscopy was used to observe mycelium morphology. 3D-QSAR was also studied.

Biological Evaluation of Selected 1,2,3-triazole Derivatives as Antibacterial and Antibiofilm Agents

2020 ◽  
Vol 20 (24) ◽  
pp. 2186-2191
Author(s):  
Lialyz Soares Pereira André ◽  
Renata Freire Alves Pereira ◽  
Felipe Ramos Pinheiro ◽  
Aislan Cristina Rheder Fagundes Pascoal ◽  
Vitor Francisco Ferreira ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Scanning Electron Microscopy ◽  
Staphylococcus Aureus ◽  
Biofilm Formation ◽  
Antimicrobial Agents ◽  
Public Health Problem ◽  
Biological Evaluation ◽  
Major Public Health Problem ◽  
Community Environments ◽  
Scanning Electron

Background: Resistance to antimicrobial agents is a major public health problem, being Staphylococcus aureus prevalent in infections in hospital and community environments and, admittedly, related to biofilm formation in biotic and abiotic surfaces. Biofilms form a complex and structured community of microorganisms surrounded by an extracellular matrix adhering to each other and to a surface that gives them even more protection from and resistance against the action of antimicrobial agents, as well as against host defenses. Methods: Aiming to control and solve these problems, our study sought to evaluate the action of 1,2,3- triazoles against a Staphylococcus aureus isolate in planktonic and in the biofilm form, evaluating the activity of this triazole through Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) tests. We have also performed cytotoxic evaluation and Scanning Electron Microscopy (SEM) of the biofilms under the treatment of the compound. The 1,2,3-triazole DAN 49 showed bacteriostatic and bactericidal activity (MIC and MBC 128 μg/mL). In addition, its presence interfered with the biofilm formation stage (1/2 MIC, p <0.000001) and demonstrated an effect on young preformed biofilm (2 MICs, p <0.05). Results: Scanning Electron Microscopy images showed a reduction in the cell population and the appearance of deformations on the surface of some bacteria in the biofilm under treatment with the compound. Conclusion: Therefore, it was possible to conclude the promising anti-biofilm potential of 1,2,3-triazole, demonstrating the importance of the synthesis of new compounds with biological activity.

scholarly journals Design, synthesis and biological evaluation of novel fungicides for the management of Fusarium DieBack disease

2019 ◽  
Vol 62 (3) ◽  
Author(s):  
Israel Bonilla Landa ◽  
Osvaldo León De la Cruz ◽  
Diana Sánchez Rangel ◽  
Randy Ortiz Castro ◽  
Benjamin Rodriguez Haas ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Antifungal Activity ◽  
Fusarium Solani ◽  
Antifungal Agents ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Dieback Disease ◽  
Synthetic Chemist ◽  
Fusarium Dieback ◽  
Synthesis And Biological Evaluation

Abstract. Fusarium Dieback, a new and lethal insect-vectored disease can host over 300 tree species including the avocado trees. This problem has recently attracted the attention of synthetic chemist not only to develop new triazol antifungal agents but also due to severe drug resistance to “classic” triazol antifungal agents. Here, a series of novel antifungal triazoles with a p-trifluoromethylphenyl moiety were synthesized and characterized by spectroscopic and spectrometric methods. Most of the target compounds synthesized showed from modest to good inhibitory activity and less phytotoxicity in comparison with the commercially available propiconazol; in particular, compounds 7 and 13 were active against both Fusarium solani and Fusarium euwallaceae. The results showed that compounds 7, 13, and 4 have great potential to be developed as new antifungal agents because of both good antifungal activity and low phytotoxicity. SAR showed that free alcohols and not O-protected compounds significantly influence the activity. Hence, a-methyl-a-1,2,4-triazole emerged as novel compound to develop new ketone-triazole-type antifungal agents for the management of Fusarium Dieback disease Resumen. Fusarium Dieback es una nueva enfermedad letal transmitida por insectos que actúan como vectores y puede atacar a más de 300 especies de árboles, incluidos los árboles de aguacate. Recientemente, este problema ha atraído la atención de los químicos sintéticos para desarrollar nuevos agentes antifúngicos triazólicos debido a la resistencia severa que desarrollan los insectos a los agentes antifúngicos triazólicos "clásicos". Durante este trabajo, se sintetizaron nuevos triazoles antifúngicos que contienen un grupo p-trifluorometilfenilo y se caracterizaron por métodos espectroscópicos y espectrométricos. La mayoría de los compuestos diana sintetizados mostraron una actividad inhibidora de modesta a buena y menos fitotoxicidad en comparación con el propiconazol que es comercialmente disponible; en particular, los compuestos 7 y 13 mostraron ser activos contra Fusarium solani y Fusarium euwallaceae. Los resultados mostraron que los compuestos 7, 13 y 4 tienen un gran potencial para desarrollarse como nuevos agentes antifúngicos debido a la buena actividad antifúngica y su baja fitotoxicidad. SAR mostró que los alcoholes libres y no los compuestos O-protegidos influyen significativamente en la actividad. Por lo tanto, el α-metil-α-1,2,4-triazol surgió como un nuevo compuesto líder para desarrollar nuevos agentes antifúngicos tipo cetona-triazol para el tratamiento de la enfermedad Fusarium Dieback.

Novel 5-chloro-pyrazole derivatives containing a phenylhydrazone moiety as potent antifungal agents: synthesis, crystal structure, biological evaluation and a 3D-QSAR study

2019 ◽  
Vol 43 (16) ◽  
pp. 6350-6360 ◽  
Author(s):  
Jian Jiao ◽  
An Wang ◽  
Min Chen ◽  
Meng-Qi Wang ◽  
Chun-Long Yang
Keyword(s):  
Crystal Structure ◽  
Structural Optimization ◽  
Fungicidal Activity ◽  
Antifungal Agents ◽  
3D Qsar ◽  
Biological Evaluation ◽  
Pyrazole Derivatives ◽  
Qsar Study

Novel 5-chloro-pyrazole derivatives containing a phenylhydrazone moiety were designed and synthesized. Some of the target compounds showed potent fungicidal activity. A 3D-QSAR study provides information for structural optimization.

Design, synthesis, antifungal activity and 3D-QSAR study of novel pyrazole carboxamide and niacinamide derivatives containing benzimidazole moiety

2019 ◽  
Vol 43 (7) ◽  
pp. 3000-3010 ◽  
Author(s):  
Wei-Jie Si ◽  
Xiao-Bin Wang ◽  
Min Chen ◽  
Meng-Qi Wang ◽  
Ai-Min Lu ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Predictive Ability ◽  
3D Qsar ◽  
Qsar Model ◽  
Qsar Study ◽  
Design Synthesis ◽  
Effective Inhibition

The synthesized pyrazole carboxamide and niacinamide derivatives containing a benzimidazole moiety showed effective inhibition of the fungus B. cinereal growth. The 3D-QSAR model was built and revealed fine predictive ability.

scholarly journals Antifungal activity of Stenotrophomonas maltophilia in Stomoxys calcitranslarvae

2014 ◽  
Vol 23 (2) ◽  
pp. 194-199 ◽  
Author(s):  
Ana Paula Rodrigues Moraes ◽  
Sandy Sampaio Videira ◽  
Vânia Rita Elias Pinheiro Bittencourt ◽  
Avelino José Bittencourt
Keyword(s):  
Electron Microscopy ◽  
Scanning Electron Microscopy ◽  
Antifungal Activity ◽  
Stenotrophomonas Maltophilia ◽  
Solid Medium ◽  
Stomoxys Calcitrans ◽  
Chain Reaction ◽  
Identification Methods ◽  
Polymerase Chain ◽  
Scanning Electron

The microbiota present in Stomoxys calcitrans larvae may assist their survival in contaminated environments through production of inhibitory substances. Bacteriological identification methods, the polymerase chain reaction (PCR) and scanning electron microscopy (SEM) were used to detect a bacterium naturally present in mucus and maceratedS. calcitrans larvae. The antifungal activity was determined based on the results from disk diffusion tests on an artificial solid medium. The bacterium was identified as Stenotrophomonas maltophilia and presented antifungal activity againstBeauveria bassiana sensu lato isolates CG 138, CG 228 and ESALQ 986. This result suggests that the larval microbiota is a factor that can compromise the use of B. bassiana s.l. fungus for biological control of S. calcitrans larvae.

Antifungal activity of naftifine against various yeasts and dermatophytes: determination of minimal inhibitory concentrations and revelation of cell wall alterations by scanning electron microscopy

1991 ◽  
Vol 37 (12) ◽  
pp. 964-970 ◽  
Author(s):  
M. Mallié ◽  
P. Butty ◽  
B. Montès ◽  
S. Jouvert ◽  
J.-M. Bastide
Keyword(s):  
Electron Microscopy ◽  
Scanning Electron Microscopy ◽  
Cell Wall ◽  
Antifungal Activity ◽  
Candida Parapsilosis ◽  
Yeast Cells ◽  
Dilution Method ◽  
Microsporum Canis ◽  
Microsporum Gypseum ◽  
Scanning Electron

The in vitro antifungal activity of naftifine, an allylamine derivative, was compared with that of econazole and clotrimazole, imidazole derivatives. The minimal inhibitory concentration (MIC) values were determined against 136 strains of yeasts (Candida albicans, Candida guilliermondii, Candida krusei, Candida parapsilosis, Candida pseudotropicalis, Candida tropicalis, Torulopsis glabrata, Malassezia furfur) and 45 strains of dermatophytes (Microsporum canis, Microsporum gypseum, Microsporum langeronii, Trichophyton mentagrophytes, Trichophyton rubrum, Epidermophyton floccosum). The fungistatic activity was evaluated by the agar dilution method, using various media: YNB (pH 6) for Candida and Torulopsis, Dixon (pH 5.6) for Malassezia, and Sabouraud (pH 6.8) for dermatophytes. The MIC was evaluated at 28–30 °C after incubation for 24–48 h for Candida and Torulopsis and for 3 days for the dermatophytes. Malassezia were incubated for 3 days at 37 °C. Naftifine was highly active against all the dermatophytes tested and moderately or weakly active against the yeasts. Candida parapsilosis was the most sensitive of all the Candida species tested. The effects of naftifine on C. parapsilosis, Mi. canis, and Tr. mentagrophytes were studied by scanning electron microscopy. Naftifine acted on C. parapsilosis causing formation of convolutions and wrinkles and defective separation between mother and daughter yeast cells. Naftifine caused alterations of the dermatophyte cell wall and particularly the hyphal filaments. These alterations were dose and time dependent. The most prominent changes seen by scanning electron microscopy were swelling, ballooning of the hyphae, and bulbiform blunt hyphae ends. Key words: naftifine, Candida, Torulopsis, Malassezia, dermatophytes.

Pathogenesis of Human Hair Defects

1974 ◽  
Vol 32 ◽  
pp. 12-13
Author(s):  
P.S. Porter ◽  
T. Aoyagi ◽  
R. Matta
Keyword(s):  
Electron Microscopy ◽  
Scanning Electron Microscopy ◽  
Human Hair ◽  
Standard Techniques ◽  
Scanning Electron

Using standard techniques of scanning electron microscopy (SEM), over 1000 human hair defects have been studied. In several of the defects, the pathogenesis of the abnormality has been clarified using these techniques. It is the purpose of this paper to present several distinct morphologic abnormalities of hair and to discuss their pathogenesis as elucidated through techniques of scanning electron microscopy.

Ultrastructural Analysis of the Salivary Glands of Gromphadorhina Portentosa (Schaum)

1977 ◽  
Vol 35 ◽  
pp. 638-639
Author(s):  
P.J. Dailey
Keyword(s):  
Electron Microscopy ◽  
Scanning Electron Microscopy ◽  
Salivary Glands ◽  
Secretory Vesicles ◽  
The Past ◽  
Transmission Electron ◽  
Means Of Transmission ◽  
Gromphadorhina Portentosa ◽  
Scanning Electron ◽  
Topographical Relief

The structure of insect salivary glands has been extensively investigated during the past decade; however, none have attempted scanning electron microscopy (SEM) in ultrastructural examinations of these secretory organs. This study correlates fine structure by means of SEM cryofractography with that of thin-sectioned epoxy embedded material observed by means of transmission electron microscopy (TEM).Salivary glands of Gromphadorhina portentosa were excised and immediately submerged in cold (4°C) paraformaldehyde-glutaraldehyde fixative1 for 2 hr, washed and post-fixed in 1 per cent 0s04 in phosphosphate buffer (4°C for 2 hr). After ethanolic dehydration half of the samples were embedded in Epon 812 for TEM and half cryofractured and subsequently critical point dried for SEM. Dried specimens were mounted on aluminum stubs and coated with approximately 150 Å of gold in a cold sputtering apparatus.Figure 1 shows a cryofractured plane through a salivary acinus revealing topographical relief of secretory vesicles.

Two- or three-way observations of the identical cell elements within the same sections by LM, TEM and/or SEM

1978 ◽  
Vol 36 (2) ◽  
pp. 82-83 ◽  
Author(s):  
Nakazo Watari ◽  
Yasuaki Hotta ◽  
Yoshio Mabuchi
Keyword(s):  
Electron Microscopy ◽  
Scanning Electron Microscopy ◽  
Transmission Electron Microscopy ◽  
Fine Structure ◽  
Light Microscopy ◽  
Thin Sections ◽  
Transmission Electron ◽  
Identical Cell ◽  
Electron Microscopes ◽  
Scanning Electron

It is very useful if we can observe the identical cell elements within the same sections by light microscopy (LM), transmission electron microscopy (TEM) and/or scanning electron microscopy (SEM) sequentially, because, the cell fine structure can not be indicated by LM, while the color is; on the other hand, the cell fine structure can be very easily observed by EM, although its color properties may not. However, there is one problem in that LM requires thick sections of over 1 μm, while EM needs very thin sections of under 100 nm. Recently, we have developed a new method to observe the same cell elements within the same plastic sections using both light and transmission (conventional or high-voltage) electron microscopes.In this paper, we have developed two new observation methods for the identical cell elements within the same sections, both plastic-embedded and paraffin-embedded, using light microscopy, transmission electron microscopy and/or scanning electron microscopy (Fig. 1).

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