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Antifungal Drug Discovery: Focus on Incrustoporin Derivatives
Silva, Luis André Vale ; Buchta, Vladimír (advisor) ; Heidingsfeld, Olga (referee) ; Hamal, Petr (referee)
1 CONCLUSIONS In the context of Medical Mycology today, the development of new more effective antifungal agents is a priority. In fact, there are still only about six drugs in use to treat invasive fungal infections, concretely the polyene amphotericin B (including its new lipidic formulations), the antimetabolite flucytosine, the triazoles fluconazole, itraconazole, and voriconazole, and the echinocandin caspofungin. Simultaneously, the incidence of invasive opportunistic mycoses has been increasing steadily with the increasing number of immunocompromised patients, caused both by HIV (human immunodeficiency virus) infection and AIDS and the development of medical techniques, particularly referring to oncology or transplant patients. In this setting, the relevance of the development of new antifungal agents and, hence, our work presented here, is easily understandable. The group of the acyloxymethylated incrustoporin derivatives is now in a higher stage of development, after being previously studied concerning structure-antifungal activity relationship and tuning of antifungal activity. Our work has shown the best derivatives from the group, compounds LNO6-22, LNO15-22, and LNO18-22, to have broad spectrum in vitro antifungal activity and high potency, inhibiting growth of a variety of pathogenic yeasts and...
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Antifungal Drug Discovery: Focus on Incrustoporin Derivatives
Silva, Luis André Vale ; Buchta, Vladimír (advisor) ; Heidingsfeld, Olga (referee) ; Hamal, Petr (referee)
1 CONCLUSIONS In the context of Medical Mycology today, the development of new more effective antifungal agents is a priority. In fact, there are still only about six drugs in use to treat invasive fungal infections, concretely the polyene amphotericin B (including its new lipidic formulations), the antimetabolite flucytosine, the triazoles fluconazole, itraconazole, and voriconazole, and the echinocandin caspofungin. Simultaneously, the incidence of invasive opportunistic mycoses has been increasing steadily with the increasing number of immunocompromised patients, caused both by HIV (human immunodeficiency virus) infection and AIDS and the development of medical techniques, particularly referring to oncology or transplant patients. In this setting, the relevance of the development of new antifungal agents and, hence, our work presented here, is easily understandable. The group of the acyloxymethylated incrustoporin derivatives is now in a higher stage of development, after being previously studied concerning structure-antifungal activity relationship and tuning of antifungal activity. Our work has shown the best derivatives from the group, compounds LNO6-22, LNO15-22, and LNO18-22, to have broad spectrum in vitro antifungal activity and high potency, inhibiting growth of a variety of pathogenic yeasts and...
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Izotopicky značené peptidy poskytující rozlišená strukturní data pomocí infračervených specter. Strukturní limity optické spektroskopie
Keiderling, T. A. ; Huang, R. ; Kubelka, J. ; Bouř, Petr ; Setnička, V. ; Hammer, R. P. ; Etienne, M. A. ; Silva, R. A. G. D. ; Decatur, S. M.
Isotopic labeling, here exemplified by 13C substitution on the amide C=O group, can allow site-specific determination of peptide conformation with IR. Examples of helix and sheet (beta-hairpin) structures are reviewed.
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