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1.
J Mycol Med ; 33(3): 101409, 2023 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-37354816

RESUMO

The increasing incidences of fungal infections among Covid-19 infected patients is a global public concern and urgently demands novel antifungals. Biopolymers like chitosan hold unique structural properties and thus can be utilized in the synthesis of biologically important scaffolds. To address the current scenario, the author's synthesized novel chitosan-azetidine derivative by adopting one-pot multicomponent reaction approach. The influence of chemical modification on the structural characteristics was investigated by means of spectroscopic techniques viz. FT-IR and 1HNMR and elemental analysis. Additionally, the authors investigated the antifungal potential of chitosan-azetidine derivative against Aspergillus fumigatus 3007 and the results indicated higher antifungal effect with an antifungal inhibitory index of 26.19%. The SEM and confocal microscopy images also reflected a significant inhibitory effect on the morphology of fungal mycelia, thus reflecting the potential of synthesized chitosan-azetidine derivativeas a potential antifungal agent.


Assuntos
Azetidinas , COVID-19 , Quitosana , Humanos , Antifúngicos/química , Quitosana/farmacologia , Quitosana/química , Espectroscopia de Infravermelho com Transformada de Fourier
2.
J Mycol Med ; 30(1): 100910, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31806380

RESUMO

The fungal diseases represent an increasing global health burden and have transformed from a rare curiosity to the leading cause of human mortality. The present manuscript reports the antifungal potential of two novel compounds possessing a carbohydrate and an imidazole moiety. Antifungal susceptibility test determined the growth inhibition potential of the synthesized compounds against Aspergillus niger 9689 and it was observed that compounds D and E gave an antifungal inhibitory index of 66.66 and 56.67% respectively. Further, ultra-structure analysis of the treated fungal mycelia through scanning electron microscope (SEM) and confocal microscopy indicated significant membrane permeability and disintegration of fungal cell membrane, thus highlighting the probable role of the synthesized compounds as inhibitors of fungal lanosterol 14α-demethylase. In silico studies corroborated with the in-vitro results, as the synthesized compounds interacted with the critical amino acids present at the active site of the fungal enzyme (lanosterol 14α-demethylase).


Assuntos
Antifúngicos , Carboidratos/química , Membrana Celular/efeitos dos fármacos , Imidazóis/química , Inibidores de 14-alfa Desmetilase/síntese química , Inibidores de 14-alfa Desmetilase/química , Inibidores de 14-alfa Desmetilase/farmacologia , Antifúngicos/síntese química , Antifúngicos/química , Antifúngicos/farmacologia , Aspergillus niger/efeitos dos fármacos , Aspergillus niger/ultraestrutura , Sequência de Carboidratos/fisiologia , Permeabilidade da Membrana Celular/efeitos dos fármacos , Humanos , Imidazóis/síntese química , Imidazóis/farmacologia , Testes de Sensibilidade Microbiana , Modelos Moleculares , Simulação de Acoplamento Molecular , Estrutura Molecular , Esterol 14-Desmetilase/metabolismo , Relação Estrutura-Atividade
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