| Full text | |
| Author(s): |
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]
Total Authors: 6
|
| Affiliation: | [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
Total Affiliations: 3
|
| Document type: | Journal article |
| Source: | Folia Microbiologica; v. 65, n. 6 AUG 2020. |
| Web of Science Citations: | 0 |
| Abstract | |
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) | |
| FAPESP's process: | 16/25028-3 - Antihistamines H3R/H4R as procognitive agents: a multitarget approach |
| Grantee: | João Paulo dos Santos Fernandes |
| Support Opportunities: | Regular Research Grants |
| FAPESP's process: | 18/03918-2 - Evaluation of the antiparasitic activity and cytotoxicity of natural products derivatives in Trypanosoma cruzi: design and synthesis of analogues potentially superior |
| Grantee: | Marina Themoteo Varela |
| Support Opportunities: | Scholarships in Brazil - Doctorate |