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Synthesis of novel papulacandin D analogs and evaluation of their antifungal po...
Bretas, Ana Carolina Oliveira; Souza, Thiago Belarmino de; Borelli, Beatriz; Johan, Suzana; Alves, Ricardo JoséSystemic fungal infections are a growing problem in contemporary medicine and few drugs are licensed for therapy of invasive fungal infections. Differences between fungi and humans, like the presence of a cell wall in fungal cells, can be explored for designing new drugs. (1,3)-β-D-glucan synthase, an enzyme that catalyzes the synthesis of (1,3)-β-D-glucan, a structural and essential component of the fungal cel...
Design and synthesis of new benzophenone derivatives with in vivo anti-inflamma...
Januário, Jaqueline Pereira; Souza, Thiago Belarmino de; Lavorato, Stefânia Neiva; Maiolini, Tatiane Cristina Silva; Domingos, Olívia da SilvaA series of novel benzophenone derivatives containing a thiazole heterocyclic nucleus were designed by molecular hybridization. Molecular docking studies have demonstrated the inhibitory potential of the designed compounds against cyclooxygenase (COX) isoenzymes. These compounds were synthesized, characterized, and evaluated for their anti-inflammatory properties by the croton oil-induced ear edema assay to exa...
A novel platinum complex containing a piplartine derivative exhibits enhanced c...
Oliveira, Maiara de Souza; Barbosa, Marília Imaculada Frazão; Souza, Thiago Belarmino de; Moreira, Diogo Rodrigo de Magalhães; Martins, Felipe TerraPiplartine (piperlongumine) is a plant-derived compound found in some Piper species that became a novel potential antineoplastic agent. In the present study, we synthesized a novel platinum complex containing a piplartine derivative cis-[PtCl(PIP-OH)(PPh3)2]PF6 (where, PIP-OH = piplartine demethylated derivative; and PPh3 = triphenylphosphine) with enhanced cytotoxicity in different cancer cells, and investigat...
Synthesis, activity and docking studies of eugenol-based glucosides as new agen...
Santos, Marcelo Henrique dos; Hipólito, Taciane Maíra Magalhães; Bastos, Guilherme Tadeu Lemos; Barbosa, Thúlio Wliandon LemosSeventeen new synthetic derivatives of eugenol (6, 8–15 and 8′‐15′) were planned following literature reports on antifungal activities of nitroeugenol and eugenol glucoside. The anti‐Candida activity of these compounds was investigated by in vitro assay and the cytotoxicity evaluation was performed with the most active compounds. The peracetylated glucosides presented better biological results than their hydrox...