FK463, a novel water-soluble echinocandin lipopeptide: synthesis and antifungal activity.
نویسندگان
چکیده
Anincreasing number of patients with marked immunosuppression as a result of transplantation, cancer and infection with Hiy has led to the increased, and widespread use of systemic antifungal agents.1} Currently available treatment is limited to 5-fluorocytosine, amphotericin B and azoles such as fluconazole and itraconazole. However, various problems effect the use of these agents. Among the major concerns are toxicity, rapid development of resistance, fungistatic effect and narrow antifungal spectrum, depending on the agent. In the search for new antifungals, fungal cell wall synthesis is an attractive target due to the presence of a number of fungi-specific enzymes,2) leading to the expectation of selective toxicity
منابع مشابه
Discovery of micafungin (FK463): A novel antifungal drug derived from a natural product lead
FR901379, which is a novel, water-soluble, echinocandin-like lipopeptide, was isolated from a microbial culture broth. It showed potent in vivo antifungal activity against Candida albicans and inhibits the synthesis of 1,3-β-glucan. However, this compound had hemolytic activity and was also less active against Aspergillus fumigatus. To overcome these shortcomings, we synthesized FR131535 bearin...
متن کاملIn vitro antifungal activity of FK463, a new water-soluble echinocandin-like lipopeptide.
The antifungal activity of FK463 against 72 recent clinical isolates of Candida albicans (24), Candida glabrata (17), Candida tropicalis (11), Candida krusei (8) and Candida parapsilosis (12) was compared with those of amphotericin B, fluconazole and itraconazole by means of a broth microdilution method specified by the National Committee for Clinical Laboratory Standards (NCCLS) document M27-A...
متن کاملCompartmental pharmacokinetics and tissue distribution of the antifungal echinocandin lipopeptide micafungin (FK463) in rabbits.
The plasma pharmacokinetics and tissue distribution of the novel antifungal echinocandin-like lipopeptide micafungin (FK463) were investigated in healthy rabbits. Cohorts of three animals each received micafungin at 0.5, 1, and 2 mg/kg of body weight intravenously once daily for a total of 8 days. Serial plasma samples were collected on days 1 and 7, and tissue samples were obtained 30 min afte...
متن کاملIn vitro activities of a new lipopeptide antifungal agent, FK463, against a variety of clinically important fungi.
The in vitro antifungal activity and spectrum of FK463 were compared with those of amphotericin B, fluconazole, and itraconazole by using a broth microdilution method specified by National Committee for Clinical Laboratory Standards document M27-A (National Committee for Clinical Laboratory Standards, Wayne, Pa., 1997). FK463 exhibited broad-spectrum activity against clinically important pathog...
متن کاملMulundocandin, an echinocandin-like lipopeptide antifungal agent: biological activities in vitro.
Mulundocandin (MCN) is an antifungal lipopeptide which belongs to the echinocandin class of antimycotic agents. MCN exhibited good in vitro activity against Candida albicans and C. glabrata isolates with MIC ranges of 0.5-4.0 microg/ml and 2.0-4.0 microg/ml, respectively. MCN also exhibited some activity against C. tropicalis isolates (MIC range 1.0-8.0 microg/ml). However, MCN was poorly activ...
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ورودعنوان ژورنال:
- The Journal of antibiotics
دوره 52 7 شماره
صفحات -
تاریخ انتشار 1999