ChemInform Abstract: cis-5-Alkyl(or Alkenyl)-3-phenyl-3(1H-imidazol-1-ylmethyl)-2-methylisoxazolidine Derivatives: In vitro Antifungal Activity and Structure-Activity Relationships.

ChemInform ◽  
1989 ◽  
Vol 20 (26) ◽  
Author(s):  
P. A. SWIFT ◽  
G. A. BENNETT ◽  
G. B. MULLEN ◽  
J. T. MITCHELL ◽  
S. D. ALLEN ◽  
...  
Holzforschung ◽  
2005 ◽  
Vol 59 (6) ◽  
pp. 620-627 ◽  
Author(s):  
Chi-Lin Wu ◽  
Shih-Chang Chien ◽  
Sheng-Yang Wang ◽  
Yueh-Hsiung Kuo ◽  
Shang-Tzen Chang

Abstract Cadinane-type sesquiterpenes have a wide spectrum of biological activity, but their use as wood preservatives and the structure-activity relationships of their derivatives have not yet been reported. A total of 13 compounds were synthesized from T-cadinol, T-muurolol, and α-cadinol and their chemical structures were confirmed by IR, MS, and 1H and 13C NMR. The antifungal properties of 16 compounds against three wood-decay fungi were evaluated in vitro. α-Cadinol showed strong antifungal activity against Lenzites betulina, Trametes versicolor, and Laetiporus sulphureus (total mean IC50 0.10 mM). Among the derivatives synthesized, 3β-ethoxy-T-muurolol (0.24 mM), 4ξH-cadinan-10β-ol (0.25 mM), 4ξH-muurolan-10β-ol (0.29 mM), and 4ξH-cadinan-10α-ol (0.25 mM) showed good antifungal activity against all fungi tested. Correlation was observed between the antifungal activity of the compounds tested and log P. Furthermore, the presence of an unsaturated double bond and oxygen-containing functional groups in the compounds plays a key role in their antifungal activity. The stereo configuration of cadinane-type sesquiterpenes also influences their antifungal activity. Understanding how the structure of natural compounds relates to their antifungal function is important and may facilitate their application as novel wood preservatives.


2005 ◽  
Vol 40 (1-2) ◽  
pp. 43-54 ◽  
Author(s):  
K. Yamunarani ◽  
R. Jaganathan ◽  
R. Bhaskaran ◽  
P. Govindaraju ◽  
R. Velazhahan

Author(s):  
Rakesh Patel ◽  
Hardik Patel ◽  
Ashok Baria

The aim of this work was to prepare and evaluate the topical carbopol gel formulation containing ketoconazole encapsulated liposomes. Ketoconazole loaded liposomes were prepared by thin film hydration technique. The prepared liposomes were incorporated into 1% carbopol gel, and the systems were evaluated for in-vitro drug release, drug retention into skin and in-vitro antifungal activity. The in-vitro permeation of ketoconazole using wistar albino rat skin from liposomal gel was compared with that of plain drug gel and also with plain drug cream containing 2% w/w of ketoconazole. The release of ketoconazole from liposomal gel was much slower than from non liposomal formulations. Gel containing liposomal ketoconazole showed maximum antifungal activity after 30 hours over plain ketoconazole gel and cream formulations.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 998
Author(s):  
Virgínia Barreto Lordello ◽  
Andréia Bagliotti Meneguin ◽  
Sarah Raquel de Annunzio ◽  
Maria Pía Taranto ◽  
Marlus Chorilli ◽  
...  

Background: Probiotic bacteria have been emerging as a trustworthy choice for the prevention and treatment of Candida spp. infections. This study aimed to develop and characterize an orodispersible film (ODF) for delivering the potentially probiotic Enterococcus faecium CRL 183 into the oral cavity, evaluating its in vitro antifungal activity against Candida albicans. Methods and Results: The ODF was composed by carboxymethylcellulose, gelatin, and potato starch, and its physical, chemical, and mechanical properties were studied. The probiotic resistance and viability during processing and storage were evaluated as well as its in vitro antifungal activity against C. albicans. The ODFs were thin, resistant, and flexible, with neutral pH and microbiologically safe. The probiotic resisted the ODF obtaining process, demonstrating high viability (>9 log10 CFU·g−1), up to 90 days of storage at room temperature. The Probiotic Film promoted 68.9% of reduction in fungal early biofilm and 91.2% in its mature biofilm compared to the group stimulated with the control film. Those results were confirmed through SEM images. Conclusion: The probiotic ODF developed is a promising strategy to prevent oral candidiasis, since it permits the local probiotic delivery, which in turn was able to reduce C. albicans biofilm formation.


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