Search Results - "Consolin Chelucci, Rafael"
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Structure‐Metabolism Relationships of Benzimidazole Derivatives with anti‐Trypanosoma cruzi Activity for Chagas Disease
Published in ChemMedChem (16-10-2024)“…This study introduces further insights from the hit‐to‐lead optimization process involving a series of benzimidazole derivatives acting as inhibitors of the…”
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2
Identification of natural cytochalasins as leads for neglected tropical diseases drug discovery
Published in PloS one (03-10-2022)“…Investigating the chemical diversity of natural products from tropical environments is an inspiring approach to developing new drug candidates for neglected…”
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3
Discovery of Arylpiperazines with Broad-Spectrum Antimicrobial Activity and Favorable Pharmacokinetic Profiles
Published in Chemistry & biodiversity (26-09-2024)“…Microorganisms can induce diseases with significant clinical implications for human health. Multidrug-resistant microorganisms have been on the rise worldwide…”
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4
2-aminobenzimidazoles for leishmaniasis: From initial hit discovery to in vivo profiling
Published in PLoS neglected tropical diseases (22-02-2021)“…Leishmaniasis is a major infectious disease with hundreds of thousands of new cases and over 20,000 deaths each year. The current drugs to treat this…”
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5
Design, Synthesis, and Pharmacological Evaluation of Novel Hybrid Compounds to Treat Sickle Cell Disease Symptoms. Part II: Furoxan Derivatives
Published in Journal of medicinal chemistry (13-09-2012)“…Phthalimide derivatives containing furoxanyl subunits as nitric oxide (NO)-donors (3a–g) were designed, synthesized, and evaluated in vitro and in vivo for…”
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6
Antiplatelet and antithrombotic activities of non-steroidal anti-inflammatory drugs containing an N-acyl hydrazone subunit
Published in Molecules (Basel, Switzerland) (17-02-2014)“…Nonsteroidal anti-inflammatory drugs (NSAIDs) 1-5 containing an N-acyl hydrazone subunit were prepared and their antiplatelet and antithrombotic activities…”
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7
Pharmacological evaluation and preparation of nonsteroidal anti-inflammatory drugs containing an N-acyl hydrazone subunit
Published in International journal of molecular sciences (04-04-2014)“…A series of anti-inflammatory derivatives containing an N-acyl hydrazone subunit (4a-e) were synthesized and characterized. Docking studies were performed that…”
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8
Pharmacological evaluation and preliminary pharmacokinetics studies of a new diclofenac prodrug without gastric ulceration effect
Published in International journal of molecular sciences (19-11-2012)“…Long-term nonsteroidal anti-inflammatory drugs (NSAIDs) therapy has been associated with several adverse effects such as gastric ulceration and cardiovascular…”
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9
Current advances in drug discovery for Chagas disease
Published in European journal of medicinal chemistry (15-07-2018)“…Chagas disease, also known as American trypanosomiasis, is one of the 17 neglected tropical diseases (NTDs) according to World Health Organization. It is…”
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10
Hit-to-lead optimization of a 2-aminobenzimidazole series as new candidates for chagas disease
Published in European journal of medicinal chemistry (15-01-2023)“…Chagas disease is a neglected tropical disease caused by Trypanosoma cruzi. Because current treatments present several limitations, including long duration,…”
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11
Structure-activity relationships of novel N -imidazoylpiperazines with potent anti- Trypanosoma cruzi activity
Published in Future medicinal chemistry (01-02-2024)“…Chagas disease is caused by the parasite , and the lack of effective and safe treatments makes identifying new classes of compounds with anti- activity of…”
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12
Synthesis and evaluation of resveratrol derivatives as fetal hemoglobin inducers
Published in Bioorganic chemistry (01-07-2020)“…[Display omitted] •New resveratrol derivatives (10a-i) with NO-donor properties.•All compounds exhibited in vivo analgesic effect.•All compounds did not induce…”
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13
Discovery of phenylsulfonylfuroxan derivatives as gamma globin inducers by histone acetylation
Published in European journal of medicinal chemistry (25-06-2018)“…N-oxide derivatives 5(a–b), 8(a–b), and 11(a–c) were designed, synthesized and evaluated in vitro and in vivo as potential drugs that are able to ameliorate…”
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14
Identification of natural cytochalasins as leads for neglected tropical diseases drug discovery
Published in PloS one (01-01-2022)“…Investigating the chemical diversity of natural products from tropical environments is an inspiring approach to developing new drug candidates for neglected…”
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15
Synthesis and evaluation of novel dapsone–thalidomide hybrids for the treatment of type 2 leprosy reactions
Published in Bioorganic & medicinal chemistry letters (15-07-2014)“…[Display omitted] We synthesized a series of novel dapsone–thalidomide hybrids (3a–i) by molecular hybridization and evaluated their potential for the…”
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