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The DOI matches its Crossref record; 8 of the 8 references it cites were found in a registry or an index.

History of the development of azole derivatives

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Maertens, J.A.·2004·Clinical Microbiology and Infection

Abstract

Until the 1940s, relatively few agents were available for the treatment of systemic fungal infections. The development of the polyene antifungals represented a major advance in medical mycology. Although amphotericin B quickly became the mainstay of therapy for serious infections, its use was associated with infusion-related side-effects and dose-limiting nephrotoxicity. The continued search for new and less toxic antifungals led to the discovery of the azoles several decades later. Ketoconazole, the first available compound for the oral treatment of systemic fungal infections, was released in the early 1980s. For almost a decade, ketoconazole was regarded as the drug of choice in nonlife-threatening endemic mycoses. The introduction of the first-generation triazoles represented a second major advance in the treatment of fungal infections. Both fluconazole and itraconazole displayed a broader spectrum of antifungal activity than the imidazoles and had a markedly improved safety profile compared with amphotericin B and ketoconazole. Despite widespread use, however, these agents became subject to a number of clinically important limitations related to their suboptimal spectrum of activity, the development of resistance, the induction of hazardous drug-drug interactions, their less than optimal pharmacokinetic profile (itraconazole capsules), and toxicity. In order to overcome these limitations, several analogues have been developed. These so-called 'second-generation' triazoles, including voriconazole, posaconazole and ravuconazole, have greater potency and possess increased activity against resistant and emerging pathogens, in particular against Aspergillus spp. If the toxicity profile of these agents is comparable to or better than that of the first-generation triazoles and drug interactions remain manageable, then these compounds represent a true expansion of our antifungal arsenal.

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Metadata

Authors
Maertens, J. A.
Venue
Clinical Microbiology and Infection
Publisher
Elsevier BV
Published
2004
Volume
10
Pages
1-10
ISSN
1198-743X (ISSN-L)
OpenAlex
W1755623111
Cited by
475
References
8
FWCI
8.68
Type
journal article
Language
en
Open access
bronze

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CoChat. (2026). Citation check: History of the development of azole derivatives. https://app.cochat.ai/papers/10.1111/j.1470-9465.2004.00841.x
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Maertens, J. A. (2004). History of the development of azole derivatives. Clinical Microbiology and Infection. https://doi.org/10.1111/j.1470-9465.2004.00841.x

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.