Synthesis of new naphthoquinones with antifungal activity.

Synthesis of new naphthoquinones with antifungal activity.

Roldi, Larissa Lopes; Greco, Sandro José; Júnior, Valdemar Lacerda; Santos, Reginaldo Bezerra dos; Castro, Eustáquio V. R. de

Abstract:

The massive emergence of fungal diseases associated with AIDS in the 1980s and the rising frequency of fatal mycoses associated with increasing use of immunosuppressive medical therapies since the 1970s stimulated research directed towards the discovery of novel antifungal agents. Azoles, allylamines and morpholine are the largest class of antifungal agents in clinical use. Their main effect is to inhibit ergosterol biosynthetic pathway. When ergosterol is depleted, the normalpermeability and fluidity of the fungal membrane is altered, with secondary consequences for membrane-bound enzymes, such as those involved in cell wall synthesis. In addition to the agents mentioned above, the 1,4-naphtoquinones, natural and synthetic, are a very interesting compound class because of the diverse biological activities present, among which, fungicide and fungistatic actions. In order to study the synergy of activities, the objective of this work consists in the synthesis of substances derived from lawsone containing the 1,2,3-triazole and morpholine rings.

The massive emergence of fungal diseases associated with AIDS in the 1980s and the rising frequency of fatal mycoses associated with increasing use of immunosuppressive medical therapies since the 1970s stimulated research directed towards the discovery of novel antifungal agents. Azoles, allylamines and morpholine are the largest class of antifungal agents in clinical use. Their main effect is to inhibit ergosterol biosynthetic pathway. When ergosterol is depleted, the normalpermeability and fluidity of the fungal membrane is altered, with secondary consequences for membrane-bound enzymes, such as those involved in cell wall synthesis. In addition to the agents mentioned above, the 1,4-naphtoquinones, natural and synthetic, are a very interesting compound class because of the diverse biological activities present, among which, fungicide and fungistatic actions. In order to study the synergy of activities, the objective of this work consists in the synthesis of substances derived from lawsone containing the 1,2,3-triazole and morpholine rings.

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DOI: 10.5151/chempro-14bmos-R0296-2

Referências bibliográficas

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Como citar:

Roldi, Larissa Lopes; Greco, Sandro José; Júnior, Valdemar Lacerda; Santos, Reginaldo Bezerra dos; Castro, Eustáquio V. R. de; "Synthesis of new naphthoquinones with antifungal activity.", p-296-296. In: In Blucher Chemistry Proceedings, São Paulo, v. 1, n. 1, Setembro.2013. São Paulo: Blucher, 2013.
ISSN 23184043, DOI 10.5151/chempro-14bmos-R0296-2