Search Results - "Varela, Marina T."
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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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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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3
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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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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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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Improving the drug-likeness of inspiring natural products - evaluation of the antiparasitic activity against Trypanosoma cruzi through semi-synthetic and simplified analogues of licarin A
Published in Scientific reports (25-03-2020)“…Neolignan licarin A ( 1 ) was isolated from leaves of Nectandra oppositifolia (Lauraceae) and displayed activity against trypomastigote forms of the etiologic…”
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Novel potent (dihydro)benzofuranyl piperazines as human histamine receptor ligands – Functional characterization and modeling studies on H3 and H4 receptors
Published in Bioorganic & medicinal chemistry (15-01-2021)“…[Display omitted] •Allylpiperazine analogues of LINS01 compounds are potent H3 receptor antagonists.•The benzofuranyl-piperazinecarboxamide 2c is a partial…”
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Antiparasitic activity of new gibbilimbol analogues and SAR analysis through efficiency and statistical methods
Published in European journal of pharmaceutical sciences (15-09-2018)“…Chagas' disease and leishmaniasis are parasitic infections enrolled among the neglected tropical diseases, which urge for new treatments. In the search for new…”
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New alkenyl derivative from Piper malacophyllum and analogues: Antiparasitic activity against Trypanosoma cruzi and Leishmania infantum
Published in Chemical biology & drug design (01-11-2017)“…Alkylphenols isolated from Piper malacophyllum (Piperaceae), gibbilimbols A and B, showed interesting activity against the parasites Trypanosoma cruzi and…”
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Profiling of LINS01 compounds at human dopamine D2 and D3 receptors
Published in Journal of chemical sciences (Bangalore, India) (01-12-2020)“…Histamine and dopamine neuronal pathways display interesting overlapping in the CNS, especially in the limbic areas, making them very attractive to designing…”
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Evaluation of the antitrypanosoma activity and SAR study of novel LINS03 derivatives
Published in Bioorganic chemistry (01-08-2019)“…[Display omitted] •LINS03 are potent anti-Trypanosoma cruzi agents.•These compounds did not disrupt the plasma membrane.•Balance between lipophilicity and…”
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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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Pyrazinoates as antiparasitic agents against Trypanosoma cruzi
Published in Archiv der Pharmazie (Weinheim) (01-11-2018)“…This work reports a repurposing study of pyrazinoic acid (1) and methyl (2), ethyl (3) and 2‐chloroethyl (4) ester derivatives with antimycobacterial activity,…”
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Synthetic Analogues of Gibbilimbol B Induce Bioenergetic Damage and Calcium Imbalance in ITrypanosoma cruzi/I
Published in Life (Basel, Switzerland) (01-02-2023)“…Chagas disease is an endemic tropical disease caused by the protozoan Trypanosoma cruzi, which affects around 7 million people worldwide, mostly in development…”
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15
Novel potent (dihydro)benzofuranyl piperazines as human histamine receptor ligands - Functional characterization and modeling studies on H 3 and H 4 receptors
Published in Bioorganic & medicinal chemistry (15-01-2021)“…Histamine acts through four different receptors (H R-H R), the H R and H R being the most explored in the last years as drug targets. The H R is a potential…”
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