Search Results - "Fernandes, João Paulo S."
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The Importance of Medicinal Chemistry Knowledge in the Clinical Pharmacist’s Education
Published in American journal of pharmaceutical education (01-03-2018)“…Objective. To show why medicinal chemistry must be a key component of the education of pharmacy students, as well as in the pharmacist’s practice. Findings…”
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Metabolite profile of Nectandra oppositifolia Nees & Mart. and assessment of antitrypanosomal activity of bioactive compounds through efficiency analyses
Published in PloS one (25-02-2021)“…EtOH extracts from the leaves and twigs of Nectandra oppositifolia Nees & Mart. shown activity against amastigote forms of Trypanosoma cruzi. These extracts…”
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Piperazine amides with desirable solubility, physicochemical and drug-like properties: Synthesis and evaluation of the anti-Trypanosoma cruzi activity
Published in Saudi pharmaceutical journal (01-07-2023)“…The absence of effective chronic treatment, expansion to non-endemic countries and the significant burden in public health have stimulated the search for novel…”
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Antihistamines H1 as Potential Anthelmintic Agents against the Zoonotic Parasite Angiostrongylus cantonensis
Published in ACS omega (16-07-2024)“…Infections caused by parasitic helminths pose significant health concerns for both humans and animals. The limited efficacy of existing drugs underscores the…”
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Synthetic Analogues of Gibbilimbol B Induce Bioenergetic Damage and Calcium Imbalance in Trypanosoma cruzi
Published in Life (Basel, Switzerland) (28-02-2023)“…Chagas disease is an endemic tropical disease caused by the protozoan , which affects around 7 million people worldwide, mostly in development countries. The…”
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Investigation of Structure–Activity Relationships for Benzoyl and Cinnamoyl Piperazine/Piperidine Amides as Tyrosinase Inhibitors
Published in ACS omega (21-11-2023)“…Melanin is a substance that plays important roles in several organisms. Its function as an antioxidant and metal-complexing agent makes tyrosinase, the key…”
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Gibbilimbol analogues as antiparasitic agents—Synthesis and biological activity against Trypanosoma cruzi and Leishmania (L.) infantum
Published in Bioorganic & medicinal chemistry letters (15-02-2016)“…[Display omitted] The essential oils from leaves of Piper malacophyllum (Piperaceae) showed to be mainly composed by two alkenylphenol derivatives:…”
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Histamine research advancements in the second year of the COVID-19 pandemic: report of the European Histamine Research Society (EHRS)
Published in Inflammation research (01-08-2022)“…In the light of cancellation of the 50th Annual Meeting of the European Histamine Research Society (EHRS) due to continuing challenges and restrictions imposed…”
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Esterification of p -Coumaric Acid Improves the Control over Melanoma Cell Growth
Published in Biomedicines (12-01-2023)“…Previous studies reported that p-coumaric acid modulates melanoma growth. Because the esterification of p-coumaric acid (p-CA) enhanced its activity as an…”
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Differential contribution of H3R antagonism by LINS01 compounds on memory, anxiety-like behaviour and spontaneous locomotor activity in healthy rats
Published in Behavioural brain research (13-01-2020)“…[Display omitted] •LINS01 compounds are promising histamine H3 receptor antagonists.•LINS01004 did not impair memory in healthy rats.•LINS01 molecules did not…”
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Coumaric acid derivatives as tyrosinase inhibitors: Efficacy studies through in silico, in vitro and ex vivo approaches
Published in Bioorganic chemistry (01-10-2020)“…[Display omitted] •The p-coumaric acid esters are inhibitors of tyrosinase.•The antimelanogenic activity is independent of radical scavenging effect.•The…”
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Toward anthelmintic drug candidates for toxocariasis: Challenges and recent developments
Published in European journal of medicinal chemistry (05-05-2023)“…Infections caused by parasitic helminths rank among the most prevalent infections of humans and animals. Toxocariasis, caused by nematodes of the genus…”
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Lethal action of Licarin A derivatives in Leishmania (L.) infantum: Imbalance of calcium and bioenergetic metabolism
Published in Biochimie (01-05-2023)“…Natural metabolites present an extraordinary chemo-diversity and have been used as the inspiration for new drugs. Considering the need for new treatments…”
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Histamine H3 receptor and cholinesterases as synergistic targets for cognitive decline: Strategies to the rational design of multitarget ligands
Published in Chemical biology & drug design (01-08-2021)“…The role of histamine and acetylcholine in cognitive functions suggests that compounds able to increase both histaminergic and cholinergic neurotransmissions…”
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The histamine H4 receptor antagonist 1-[(5-chloro-2,3-dihydro-1-benzofuran-2-yl)methyl]-4-methyl-piperazine(LINS01007) prevents the development of DSS-induced colitis in mice
Published in International immunopharmacology (30-05-2024)“…•A new H4R antagonist prevents the development of DSS-induced colitis in mice.•Histological signs were significantly reduced in animals treated with…”
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Multitargeting approaches to cognitive impairment: Synthesis of aryl-alkylpiperazines and assessment at cholinesterases, histamine H3 and dopamine D3 receptors
Published in Bioorganic & medicinal chemistry (15-01-2023)“…[Display omitted] Multitargeting ligands on enzymes and receptors may generate a profile for a potential treatment of cognitive impairment. Considering this, a…”
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Optimization of physicochemical properties is a strategy to improve drug-likeness associated with activity: Novel active and selective compounds against Trypanosoma cruzi
Published in European journal of pharmaceutical sciences (01-04-2022)“…Trypanosoma cruzi is the causing agent of Chagas disease, a parasitic infection without efficient treatment for chronic patients. Despite the efforts, no new…”
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Bioisosteric modification on benzylidene‐carbonyl compounds improved the drug‐likeness and maintained the antifungal activity against Sporothrix brasiliensis
Published in Chemical biology & drug design (01-03-2022)“…Considering the emergence of antifungal resistance on Sporothrix brasiliensis, we aimed to assess new benzylidene‐carbonyl compounds against feline‐borne S…”
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Coumaric acid analogues inhibit growth and melanin biosynthesis in Cryptococcus neoformans and potentialize amphotericin B antifungal activity
Published in European journal of pharmaceutical sciences (01-10-2020)“…•Novel coumaric acid analogues with fungal tyrosinase inhibitory activity are described.•These compounds also cause growth arrest and melanization inhibition…”
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Novel potent vasodilating agents: Evaluation of the activity and potency of LINS01005 and derivatives in rat aorta
Published in European journal of pharmaceutical sciences (15-02-2020)“…•LINS01005 is a potent vasodilating agent in rat thoracic aortha.•Compounds are more potent in SHR than Wistar rat's vessels.•N-Phenylpiperazine motif is…”
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