Navegando por Autor "Cordeiro, Cleydson Finotti"

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Synthesis and antimicrobial activity of molecular hybrids based on eugenol and chloramphenicol pharmacophores.
(2023) Oliveira, Lucas Martins; Siqueira, Fallon dos Santos; Silva, Michelle T.; Machado, José Vaz Cardoso; Cordeiro, Cleydson Finotti; Diniz, Lívia de Figueiredo; Campos, Marli Matiko Anraku de; Franco, Lucas Lopardi; Souza, Thiago Belarmino de; Hawkes, Jamie Anthony; Carvalho, Diogo Teixeira
In the constant search for new pharmacological compounds, molecular hybridisation is a well-known technique whereby two or more known pharmacophoric subunits are combined to create a new “hybrid” compound. This hybrid is expected to maintain the characteristics of the original compounds whilst demonstrating improvements to their pharmacological action. Accordingly, we report here a series of molecular hybrid compounds based upon eugenol and chloramphenicol pharmacophores. The hybrid compounds were screened for their in vitro antimicrobial potential against Gram-negative and Gram-positive bacteria and also rapidly growing mycobacteria (RGM). The results highlight that the antimicrobial profiles of the hybrid compounds improve in a very clear fashion when moving through the series. The most prominent results were found when comparing the activity of the hybrid compounds against some of the multidrug-resistant clinical isolates of Pseudomonas aeruginosa, methicillin-resistant clinical isolates of Staphylococcus aureus (MRSA) and clinical isolates of rapidly growing mycobacteria.
Synthesis of eugenol-derived glucosides and evaluation of their ability in inhibiting the angiotensin converting enzyme.
(2020) Alvarenga, Dalila Junqueira; Matias, Laira Maria Faria; Cordeiro, Cleydson Finotti; Souza, Thiago Belarmino de; Lavorato, Stefânia Neiva; Pereira, Marília Gabriella Alves Goulart; Dias, Danielle Ferreira; Carvalho, Diogo Teixeira
We report here a series of glucosides which are active as inhibi tors of the angiotensin converting enzyme (ACE). They are struc turally related to the natural compound eugenol and exhibited significant inhibition values. Their syntheses were expeditious and we could obtain informative docking plots of them complexed to this enzyme. A glucoside derived from eugenol, carrying a carbox ylic group in the aglycone, was the most active of them (with an IC50 of 0.4 mM) and showed good binding energies in docking studies with ACE. Moreover, computational prediction of toxicity risks, physicochemical properties and drug score show that the glucoside derivative of eugenol is a suitable compound for opti misation studies aimed at finding new drug candidates.