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Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 30 for “"Azoles"”.
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Comparative efficacy of azole compounds targeting sterol 14-demethylase against multiple isolates of Acanthamoeba castellanii and polyphaga
… an attractive drug target in Acanthamoeba. Azoles are an antifungal medication that target the cytochrome P450 enzyme sterol 14-demethylase, this enzyme is essential in the ergosterol pathway and its inhibition results in the loss of membrane stability and cell death. In this study five …
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Investigating FDA-Approved Drugs for Treatment of Multidrug-Resistant Neisseria gonorrhoeae
… were further investigated in vitro. Of the three azoles, ravuconazole displayed the most potent activity against N. gonorrhoeae clinical isolates. The time-kill assay revealed that the three azoles showed bactericidal activity. All three azole drugs showed a low frequency of resistance. Besides, …
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Investigating MCE Chemical Library Drugs for Combinational Therapies for Clinical Aspergillus fumigatus isolates
… increased resistance and rising mortality rates. Azoles are utilized as primary treatment options for Aspergillus fumigatus infections such as voriconazole (VRC), itraconazole (ITC), and posaconazole (POS) with a reserve of Amphotericin B (AmB). In the past two decades, the emergence of resistance …
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I. Multicatalysis: Development of a BiOTf₃-catalyzed Nucleophilic Addition/Hydrofunctionalization Reaction in the Synthesis of Complex Heterocycles; . . .
… as well as substituted pyridines. In the case of azoles, arylation probably proceeds via a mechanism different to that of C5 arylations; the phosphine ligand stabilizes catalytic intermediates, affording efficient C2 arylation of azoles. In the case of pyridine, the major issue is that of catalyst …
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Discovery and development of novel antifungal agents for the treatment of Candida auris infections
… to three main classes of antifungal drugs: azoles, polyenes, and echinocandins. The emergence of new fungal species, such as Candida auris, which displays high resistance and mortality rates (30-60%), has further complicated treatment efforts. Thus, there is a critical need for new …
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Developing novel drug combinations for treatment of invasive fungal infections
… are restricted to three classes of antifungals: Azoles, polyenes, and echinocandins. The emergence of new fungal species, especially C. auris, marked by high resistance profiles and increased mortality rates (30-60%), has further exacerbated the limitations in its therapeutic options. This …
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Genetically Engineered Wound Dressing for Sensing and Treating Candida albicans Infections in Diabetic Foot Ulcers
… Candida infections are typically treated with azoles like fluconazole. There is an unmet need to develop new strategies to detect and treat Candida infections. In this work, we developed hydrogel-based Engineered Living Materials (ELMs) as an antifungal wound dressing. Additionally, to increase …
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Novel Determinants That Influence Azole Susceptibility in Candida glabrata and Candida albicans
… class of currently available antifungals - the azoles.</p> <p>Other available antifungals have associated toxicities, are not available as oral dosage forms or are cost prohibitive. As multidrug resistant <em>C. glabrata </em>have been reported, the need to find ways to overcome resistance to …
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Targeting Coenzyme A Biosynthesis for Antifungal Development.
… efficacy of the available antifungal drugs: the azoles, echinocandins, and amphotericin B. Approximately one-third of patients with disseminated Candida infections are non-responsive to treatment with the azoles, and favorable response rates are just 52-73% for the echinocandins and just 62% for …
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Targeting CYP5122A1 and CYP51 for the Inhibition of Ergosterol Biosynthesis in Trypanosomatids
… the antileishmanial effect of antifungal azoles in vitro. Dual inhibitors of CYP51 and CYP5122A1, e.g., clotrimazole and posaconazole, possess superior antileishmanial activity against L. donovani promastigotes whereas CYP51-selective inhibitors, e.g., fluconazole and voriconazole, have …
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Signal Transduction and Transcriptional Regulation Pathways Essential for Azole Resistance in Candida albicans
… Candida infections, including OPC. However, the azoles are fungistatic against C. albicans and therefore have limited efficacy against this organism, especially for immunocompromised patients. In C. albicans, the transcription factor Upc2 is central to the regulation of ergosterol biosynthesis. …
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ERG11-Mediated Azole Resistance in Candida albicans
… available for systemic antifungal treatment, the azoles are the most suitable option for the long treatment periods sometimes required for antifungal prophylaxis and therapy. As the azoles are fungistatic to <em>Candida</em> species, the lengthy and repeated treatment courses have resulted in …
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Comparative structural analysis of cytochrome P450 family CYP51 in the genus Cryptococcus
… with nine ligands (three substrates and six azoles) performed by Rosetta docking using 10 000 combinations for each of the CYP51-ligand complex (12 CYP51s x 9 ligands =108 complexes) and hierarchical agglomerative clustering were used for selecting the complexes. A web application for …
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Functional Characterisation of the Eukaryotic Translation Elongation Factor 1Bγ in Aspergillus fumigatus; A Proteomic Systems Approach
… this study as surface (1,3)-β-glucan sequesters azoles preventing entry into the cell. Overall, this work highlights the diverse roles of A. fumigatus elfA, with respect to protein synthesis, oxidative stress and actin cytoskeleton organisation. In addition to this, the advantages of combining …
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The Molecular Mechanisms of Antifungal Drug Resistance In Pathogenic Fungi
… mostly in immune-compromised individuals. Azoles are the most common antifungals used in treating these infections. The most significant mechanisms of azole resistance include alterations or overexpression of the target enzyme, and overexpression of at least three distinct efflux pumps. …
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Efficacy and Safety of Pharmacological Treatments of Chagas Disease
… or Nifurtimox, two studies also tested azoles, Posaconazole or E1224 (Ravucanazole). Of the four trypanocidals, BNZ was shown to be the most efficacious in both types of studies. POS and E1224 both had an antiparasitic effect during the course of treatment, but the effect was not …
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The use of glutathione in canine itraconazole-associated hepatotoxicity
… sterol 14α-demethylase. The most commonly used azoles in small animal veterinary medicine are itraconazole (ITZ), fluconazole (FCZ), and ketoconazole (KTZ). Owing to its greater selectivity for fungal ergosterol over mammalian cholesterol, ITZ has fewer adverse effects than KTZ. Additionally, it …
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Exploiting fitness trade-offs to prevent antifungal drug resistance
… Resistance to this agent sensitizes fungi to azoles and bears severe fitness costs, reminiscent of the case of AmB.
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Elucidation and control of substrate recognition during RiPP biosynthesis
… Ser, or Thr to form azoline heterocycless (or azoles upon oxidation). The catalytic unit of the cyclodehydratase is a YcaO-family protein which is often accompanied by a partner protein from the E1-like superfamily (depending on the of type cyclodehydratase). Although primarily known for …
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Endosomal Trafficking as a Determinant of Antifungal Tolerance in the Pathogenic Fungus Candida albicans
… mutant was able to grow in the presence of the azoles despite depletion of cellular ergosterol. This phenotype resembles an exaggerated form of azole tolerance known as ‘trailing growth’, which has been described for some clinical isolates. In contrast, the vps21∆/∆ mutant is hypersensitive to …
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