Celso de Oliveira Rezende Júnior

Effects of Mono‐ and Dicapsaicinoid Functionalization on the Physicochemical Properties and Antimicrobial Photodynamic Activity of Protoporphyrin IX

Ieda Vieira da Cunha, Gabriel G. Caléfi, Nágela Bernadelli Sousa Silva, Júlia Gomes Teixeira et autres

Antimicrobial photodynamic therapy (aPDT) is a promising alternative for combating multidrug-resistant bacteria and overcoming limitations of conventional antimicrobial treatments. To improve aPDT performance, two Protoporphyrin IX (PpIX) derivatives functionalized with one or two capsaicin fragments were synthesized and biologically evaluated. Their physicochemical, …

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Piperazine and Morpholine Protoporphyrin IX Derivatives Intensify Biomolecules Oxidation and Phototoxicity in Triple‐Negative Breast Cancer

Maynne Duarte Suriani Franco, Thibault Joseph William Jacques Dit Lapierre, Tarcisio Paiva Mendonça, Luiz Felipe Fernandes Peixoto et autres

Photodynamic therapy (PDT) is a clinically established approach that relies on the localized generation of reactive oxygen species (ROS) mediated by a photosensitizer (PS), light, and molecular oxygen. Protoporphyrin IX (PpIX) is an approved PS; however, its intracellular retention is limited, factor …

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Identification of a Benzenesulfonylpiperazine Derivative With In Vivo Efficacy Against Visceral Leishmaniasis

Thibault Joseph William Jacques Dit Lapierre, Mariza Gabriela Faleiro de Moura Lodi Cruz, Guilherme Freitas de Lima Hercos, Rafael Consolin Chelucci et autres

Benzenesulfonylpiperazines have been previously identified as a promising class against Chagas disease and leishmaniasis, two parasitic neglected tropical diseases. Thus, the pharmacokinetic profile of two potential leads against visceral leishmaniasis was assessed in vitro. Both lead candidates 1 and 2 exhibited a …

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Hit‐To‐Lead Optimization of a Pyridylpiperazine Class Against Malaria: Pharmacokinetic Profile and In Vivo Efficacy of Optimized Compounds

Douglas Davison da Silva Oliveira, Duarte Eduardo Pereira, Rafael Consolin Chelucci, Simone Michelan et autres

Malaria remains a significant global health challenge caused by Plasmodium parasites. Current antimalarial treatment strategies face mounting challenges due to the rapid development of drug resistance. This work aimed at the hit-to-lead optimization of a pyridylpiperazine class by evaluating the in vitro …

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Discovery of an efficacious 2-ethyl-4-phenylthiazole derivative against acute Chagas disease via multiparametric hit-to-lead optimization and in vivo efficacy

Thibault Joseph William Jacques Dit Lapierre, Daniela de Melo Resende, Felipe da Silva Mendonça de Melo, Alexandra Maria dos Santos Carvalho et autres

This work describes the hit-to-lead optimization of the 2-ethyl-4-phenylthiazole class against Trypanosoma cruzi, the causative agent of Chagas disease. Compound LC-6 (1), previously identified in silico and in vitro against epimastigotes, was confirmed here as an antichagasic hit due to its sub-micromolar …

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Advancements in diverse chemical scaffolds for antimalarial drug discovery: a ten-year hit-to-lead retrospective

Marcelo Augusto Pereira Januário, Douglas Davison da Silva Oliveira, Flávio Luis Cardoso Silveira, Júlia Oliveira Carvalho et autres

Malaria remains one of the most devastating parasitic diseases worldwide, accounting for hundreds of millions of cases and significant mortality annually. Despite the availability of therapeutic interventions, the efficacy of current pharmacological treatments is increasingly compromised by the emergence and spread of …

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Furanocarboxamide Derivative Against Congenital Toxoplasmosis: Synthesis, Bioactivity, ADME Profile and in silico Insights

Júlia O. Carvalho, Ana Paula C. Procópio, Marcos Paulo Oliveira Almeida, Beatriz A. Vasconcelos et autres

Congenital toxoplasmosis remains a significant therapeutic challenge within the spectrum of Toxoplasma gondii infections is estimated about 190,000 cases per year, with a considerable infection rate worldwide (ca. 29%). This study describes the synthesis and pharmacological evaluation of compound 1, a furanocarboxamide …

Hit-to-Lead Studies of Pyrazinylpiperazines against Visceral Leishmaniasis: Pharmacokinetic Profile and In Vivo Efficacy of Potent Compounds against Leishmania infantum

Thibault Joseph William Jacques Dit Lapierre, Mariza Gabriela Faleiro de Moura Lodi Cruz, Gisele Barbosa, Analu R. Costa et autres

High Resolution Image Download MS PowerPoint Slide As part of the hit-to-lead optimization of antileishmanial pyrazinylpiperazines, the Absorption, Distribution, Metabolism, and Excretion (ADME) properties of the initial hit and five candidates for in vivo studies were assessed in vitro . These candidates, …

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Benzothiazole derivatives as inhibitors of chikungunya virus replicative cycle

Shiraz Feferbaum-Leite, Natasha Marques Cassani, Uriel Enrique Aquino Ruiz, Renieidy Flávia Clemente Dias et autres

Aims Chikungunya virus (CHIKV) is the agent of chikungunya fever (CHIKF), a reemerging disease prevalent in tropical regions. With no licensed treatments available, identifying effective antiviral compounds is critical. This study evaluates the antiviral potential of 20 synthetic sulfonamide derivatives against CHIKV.Methodology …

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Protoporphyrin IX conjugated to piperazine or morpholine: Photophysical properties and photodynamic activity

Maynne Duarte Suriani Franco, Thibault Joseph William Jacques Dit Lapierre, Ana Clara Cassiano Martinho, Naiara Cristina Bessas et autres

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Indole Derivatives as Promising Anti‐Dengue Agents: A Review of Recent Advances

Marcelo Augusto Pereira Januário, Celso de Oliveira Rezende Júnior, Ian Castro‐Gamboa

Dengue, a mosquito-borne disease transmitted by Aedes mosquitoes, is a significant global health concern. Despite extensive research, effective treatments remain limited. The indole nucleus, known for its diverse pharmacological properties, has emerged as a promising scaffold for anti-dengue drug discovery. This review …

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Photosensitizer associated with efflux pump inhibitors as a strategy for photodynamic therapy against bacterial resistance

Ieda Vieira da Cunha, Douglas Davison da Silva Oliveira, Gabriel G. Caléfi, Nágela Bernadelli Sousa Silva et autres

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