ABSTRACT
Objective:To investigate the rationality of anti-fungal agents for deep fungal infection used in one hospital and the effects of national rectification of antimicrobial drugs. Methods: The retrospective analysis method was used to survey the inpatients administrated anti-fungal agents for deep fungal infection from April 2010 to Mard 2012, and assessed the rationality. Results:The ir-rational utilization of anti-fungal agents for deep fungal infection included loading dosage lack during the treatment,inappropriate loading dosage and administration frequency. The irrational utilization of anti-fungal agents for deep fungal infection was decreased significantly (P<0. 05)after the national rectification of antimicrobial drugs. Conclusion:After the national rectification of antimicrobial drugs, the hospital can amtrol the irrational use of anti-fungal agents to some extent, while still needs more management and education.
ABSTRACT
Objective: To design and synthesize novel tetrahydroisoquinolines with anti-fungal activities. Methods: 3,4-dimethoxyphenylethylamine was taken as the template and the title compounds were synthesized through Pictet-Spengler reaction, neutralization reaction, substitution, hydrolysis, and acylation. Results: Twelve title compounds were obtained and all of them were firstly reported. Besides, all the target compounds had anti-fungal activities. The anti-fungal activities of compounds 6-8 and 10-12 were similar to or stronger than that of fluconazole's. Conclusion: Title compounds obtained in this study belong to a new type of anti-fungal agent, which deserves further study.
ABSTRACT
Objective: To investigate the anti-fungal activities of 20 tetralin compounds in vitro. Methods: We adopted the M27-A project recommended by the National Committee for Clinical Laboratory Standard (NCCLS). Tetralin compounds were tested and selected with several candidal strains and non-candidal strains with different susceptibilities to fluconazole. After obtaining the susceptibility results, we plotted the time-growth curves of several typical tetralin compounds, including compound 22-1, 31-1 and their muriate 22, 31, as well as compound 34-1, 26-1 and their bromate 34, 26. The combination effects of compound 22, 26, 34, 31-1 with other anti-fungal agents (with different structures) were also determined. Results: The 20 tetralin compounds were proven to have different degrees of anti-fungal activities. Compound 31-1 had a stronger anti-fungal activity to FLC-susceptible strains than fluconazole did, and its effect lasted for over 54 h at the concentration of 6 μg/ml. Compounds 22-1 and 22 markedly suppressed the growth of Candida albicans, Candida parapsilosis, and Trichophyton rubrum, with all the MIC50 values less than 0.125 μg/ml. Time-growth curves indicated that the anti-fungal activity of 22-1 on fluconazole-resistant strain was more powerful than that of ketoconazole. Furthermore, tetralin compounds had a synergistic effect with terbinafine and berberine on fluconazole-resistant strains. Conclusion: Tetralin compounds have powerful anti-fungal activities and their structures are different from those of other anti-fungal agents currently used, which provide a basis for developing new anti-fungal agents.