Benzylidene-carbonyl compounds are active against itraconazole-susceptible and itraconazole-resistantSporothrix brasiliensis

Autor(es)

Waller, Stefanie Bressan ^{[1, 2]} ; Cleff, Marlete Brum ^[2] ; Ripoll, Marcia Kutscher ^[1] ; Araujo Meireles, Mario Carlos ^[1] ; Varela, Marina Themoteo ^[3] ; Fernandes, Joao Paulo dos S. ^[3]

Afiliação do(s) autor(es)

^[1] Univ Fed Pelotas, Fac Vet, Dept Prevent Vet, BR-96010900 Pelotas, RS - Brazil

^[2] Univ Fed Pelotas, Fac Vet, Dept Vet Clin, BR-96010900 Pelotas, RS - Brazil

^[3] Fed Univ Sao Paulo UNIFESP, Inst Environm Chem & Pharmaceut Sci, Dept Pharmaceut Sci, BR-09913030 Diadema, SP - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Folia Microbiologica; v. 65, n. 6 AUG 2020.
• Citações Web of Science: 0

Resumo

We evaluated the antifungal activity of benzylidene-carbonyl compounds (LINS03) based on the structure of gibbilimbol fromPiper malacophyllumLinn. Five analogues (1-5) were synthetized following a classic aldol condensation between an aromatic aldehyde and a ketone, under basic conditions. These were tested against itraconazole-susceptible (n = 3) and itraconazole-resistant (n = 5) isolates ofSporothrix brasiliensisby M38-A2 guidelines of CLSI. All of them were fungistatic (MIC ranged of 0.11-0.22 mg/mL (1); 0.08-0.17 mg/mL (2); 0.05-0.1 mg/mL (3); 0.04-0.33 mg/mL (4); and 0.04-0.3 mg/mL (5)), highlighting compounds2and3. As fungicidal, compounds1and2were highlighted (MFC ranged of 0.22-0.89 mg/mL and 0.08-1.35 mg/mL, respectively), compared with the remaining (0.77-> 3.08 mg/mL (3); 0.08-> 2.6 mg/mL (4); and 0.59-> 2.37 mg/mL (5)). The inhibitory activity was related to the benzylidene-carbonyl, whereas the phenol group and the low chain homolog seems to contribute to some extent to the fungicidal effect. Compound2highlighted due to the considerable fungistatic and fungicidal activities, including itraconazole-resistantSporothrix brasiliensis. These findings support the potential usefulness of benzylidene-carbonyl compounds as promising prototypes for the development of antifungal against sporotrichosis bySporothrix brasiliensis, including against itraconazole-resistant isolates. (AU)

• Processo FAPESP: 16/25028-3 - Anti-histamínicos H3R/H4R como agentes pró-cognitivos: uma abordagem multialvo
• Beneficiário: João Paulo dos Santos Fernandes
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 18/03918-2 - Avaliação da atividade antiparasitária e da citotoxicidade de derivados de produtos naturais em Trypanosoma cruzi: planejamento e síntese de análogos potencialmente superiores
• Beneficiário: Marina Themoteo Varela
• Modalidade de apoio: Bolsas no Brasil - Doutorado