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New Antifungal Agents (new + antifungal_agent)

Distribution by Scientific Domains
Medical Sciences63%
Chemistry36%

Selected Abstracts

ChemInform Abstract: Substituted Indoloquinolines as New Antifungal Agents.

CHEMINFORM, Issue 21 2002
Seth Y. Ablordeppey
Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source]

Fatal peripheral neuropathy following FLA chemotherapy

INTERNATIONAL JOURNAL OF LABORATORY HEMATOLOGY, Issue 4 2004
W. L. Osborne
Summary We discuss a case with significant progressive peripheral neurological deterioration following administration of both fludarabine and cytarabine as part of the FLA (fludarabine and cytarabine) regime. Of particular interest is that toxicity only occurred during the second course of FLA and sixth course of Ara-C containing chemotherapy. At this point, a new antifungal agent had been commenced, suggesting a possible drug interaction enhancing the risk of known neurological toxicity with this regime. [source]

Synthesis of isotopically labelled [3- 14C]- and [3,3- 2H2]-5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2690), a new antifungal agent for the potential treatment of onychomycosis

JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, Issue 4 2007
Stephen J. Baker
Abstract 5-Fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2690) is a new antifungal agent for the potential treatment of onychomycosis. During the preclinical development phase, it was necessary to synthesize the radioisotope [3- 14C]-5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole and the deuterium isotope [3,3- 2H2]-5-fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole for in vitro studies. We report the synthesis of these two isotopically labelled derivatives. Copyright © 2007 John Wiley & Sons, Ltd. [source]

In vitro susceptibility testing in fungi: a global perspective on a variety of methods

MYCOSES, Issue 1 2010
Cornelia Lass-Flörl
Summary Candida and Aspergillus species are the most common causes of invasive fungal infections in immunocompromised patients. The introduction of new antifungal agents and recent reports of resistance emerging during treatment have highlighted the need for in vitro susceptibility testing. For some drugs, there is a supporting in vitro,in vivo correlation available from studies of clinical efficacy. Both intrinsic and emergent antifungal drug resistance are encountered. Various testing procedures have been proposed, including macrodilution and microdilution, agar diffusion, disk diffusion and Etest. Early recognition of infections caused by pathogens that are resistant to one or more antifungals is highly warranted to optimise treatment and patient outcome. [source]

In vitro susceptibility-testing in Aspergillus species

MYCOSES, Issue 5 2008
Cornelia Lass-Flörl
Summary Aspergillus species are the most common causes of invasive mould infections in immunocompromised patients. The introduction of new antifungal agents and recent reports of resistance emerging during treatment of Aspergillus infections have highlighted the need for in vitro susceptibility-testing. Various testing procedures have been proposed, including macrodilution and microdilution, agar diffusion, disc diffusion and Etest. At present, one of the most widely used assays is the M38-A reference method for filamentous fungi, published by the Clinical Laboratory Standard Institute and the Etest. Recently, the European Committee on Antimicrobial Susceptibility-testing (EUCAST) has charged its Antifungal Susceptibility-testing Subcommittee (AFST-EUCAST) with the preparation of new guidelines for in vitro susceptibility-testing of antifungals against Aspergillus spp. (EUCAST-AFST-ASPERGILLUS) defining breakpoints. This paper reviews the available methods for antifungal susceptibility-testing in Aspergillus spp. as well as the scant data regarding the clinical implications of in vitro testing. [source]

Antifungal activity of Mahonia aquifolium extract and its major protoberberine alkaloids

PHYTOTHERAPY RESEARCH, Issue 7 2003
Anna Vollekovį
Abstract The crude extract of Mahonia aquifolium (Berberidaceae) stem bark and its components berberine, palmatine and jatrorrhizine were screened for their inhibitory activity against a variety of dermatophytes and two Candida species of human origin using the in vitro dilution agar plate method. Jatrorrhizine was found to be the most effective against all fungal species tested (MIC ranges from 62.5 to 125 µg/mL), while the crude extract, berberine, and palmatine exhibited only marginal activity (MIC 500 to , 1000 µg/mL). Dermatophytes were more susceptible to jatrorrhizine than yeasts, and Scopulariopsis brevicaulis appeared the least sensitive species to all the compounds tested. The effects of the alkaloids were compared with those of .uconazole and bifonazole for which the MIC ranges were 12.5 to >100 µg/mL. Our results suggest that jatrorrhizine may serve as a leading compound for further studies to develop new antifungal agents with highly potent antifungal activity and low host toxicity. Copyright © 2003 John Wiley & Sons, Ltd. [source]

Synthesis and Antifungal Activity of 1-Aryl-3-phenethylamino-1-propanone Hydrochlorides and 3-Aroyl-4-aryl-1-phenethyl-4-piperidinols

ARCHIV DER PHARMAZIE, Issue 5 2010
Ebru Mete
Abstract Mono-Mannich bases, 1-aryl-3-phenethylamino-1-propanone hydrochlorides, 1a, 2a, 3a, 4a, 5a, 6a, 7a, 8a, 9a, and semi-cyclic mono-Mannich bases, 3-aroyl-4-aryl-1-phenethyl-4-piperidinols, 1b, 2b, 3b, 4b, 5b, 6b, 7b, 8b, 9b, were synthesized by a non-classical Mannich reaction. The aryl part was: C6H5 for 1a, 1b; 4-CH3C6H4 for 2a, 2b; 4-CH3OC6H4 for 3a, 3b; 4-ClC6H4 for 4a, 4b; 4-FC6H4 for 5a, 5b; 4-BrC6H4 for 6a, 6b; 2,4-(Cl)2C6H3 for 7a, 7b; 4-NO2C6H4 for 8a, 8b; and C4H3S(2-yl) i. e., 2-thienyl for 9a, 9b. Piperidinol compounds 2b, 3b, 4b, 5b, 7b, 8b, and 9b are reported here for the first time. The synthesized compounds were tested against seven types of plant pathogenic fungi and three types of human pathogenic fungi using the agar dilution assay. Itraconazole was tested against Candida parapsilosis as the reference compound, while Nystatin was tested as the reference compound against the other fungi. Compounds 1a, 1b, 2a, 4a, 4b, 5a, 5b, 6a, 7a, 8a, 9a, and 9b can be selected as model compounds to develop new antifungal agents against the human pathogen Microsporum canis. Compounds 8a and 8b, which had a similar antifungal activity compared with the reference compound Nystatin against the plant pathogen Aspergillus flavus, can serve as model compounds to develop new antifungal agents to solve agricultural problems. [source]

Candidemia in patients with hematologic malignancies in the era of new antifungal agents (2001-2007)

CANCER, Issue 20 2009
Stable incidence but changing epidemiology of a still frequently lethal infection
Abstract BACKGROUND: The incidence, epidemiology, Candida species distribution, resistance patterns, and outcome of candidemia in high-risk hematologic malignancy and/or stem cell transplantation patients have not been extensively described since the introduction of new antifungal agents. METHODS: In this retrospective study, the authors reviewed the medical records and microbiologic data of hematologic malignancy patients with candidemia at The University of Texas M. D. Anderson Cancer Center from March 2001 to February 2007. RESULTS: The authors analyzed 173 episodes of candidemia (170 patients), 125 (72%) of which were breakthrough cases after prior antifungal agents, mainly fluconazole (28 [22%]), caspofungin (25 [20%]), and voriconazole (18 [14%]). The incidence of candidemia (per 100,000 inpatient days) remained relatively stable, from 13.9 in 2001 to 19.2 in 2006. However, compared with the findings of previous studies at the authors' institution, the frequency of Candida glabrata and C. krusei infection decreased (to 5% and 17%, respectively) and C. parapsilosis (24%) and C. tropicalis (21%) increased. C. parapsilosis fungemia was associated with prior caspofungin use (P < .001). The overall 30-day crude mortality rate was 38%, and the attributable mortality rate was 19%, similar to previous findings at the authors' institution. The Candida species associated with the highest mortality rate was C. glabrata. CONCLUSIONS: Despite the widespread use of antifungal prophylaxis and the introduction of new antifungal agents, the incidence and associated mortality rates of candidemia remained stable in high-risk hematologic malignancy patients. However, its epidemiological characteristics have shifted, with C. parapsilosis and C. tropicalis becoming more common. Cancer 2009. © 2009 American Cancer Society. [source]

Microbial natural products as a source of antifungals

CLINICAL MICROBIOLOGY AND INFECTION, Issue 1 2003
M. F. Vicente
The vast number and variety of chemotherapeutic agents isolated from microbial natural products and used to treat bacterial infections have greatly contributed to the improvement of human health during the past century. However, only a limited number of antifungal agents (polyenes and azoles, plus the recently introduced caspofungin acetate) are currently available for the treatment of life-threatening fungal infections. Furthermore, the prevalence of systemic fungal infections has increased significantly during the past decade. For this reason, the development of new antifungal agents, preferably with novel mechanisms of action, is an urgent medical need. A selection of antifungal agents in early stages of development, produced by micro-organisms, is summarized in this review. The compounds are classified according to their mechanisms of action, covering inhibitors of the synthesis of cell wall components (glucan, chitin and mannoproteins), of sphingolipid synthesis (serine palmitoyltransferase, ceramide synthase, inositol phosphoceramide synthase and fatty acid elongation) and of protein synthesis (sordarins). In addition, some considerations related to the chemotaxonomy of the producing organisms and some issues relevant to antifungal drug discovery are also discussed. [source]