201996-24-9Relevant academic research and scientific papers
Trypanosoma cruzi Malic Enzyme Is the Target for Sulfonamide Hits from the GSK Chagas Box
Bruder, Marjorie,Cordeiro, Artur T.,Do Nascimento Faria, Jessica,Eufrásio, Amanda G.,Fagundes, Michelle,Mercaldi, Gustavo F.,Mota, Sabrina G. R.,Ranzani, Americo T.
, p. 2455 - 2471 (2021/08/06)
Chagas disease, an infectious condition caused by Trypanosoma cruzi, lacks treatment with drugs with desired efficacy and safety profiles. To address this unmet medical need, a set of trypanocidal compounds were identified through a large multicenter phen
USE OF DDX3 INHIBITORS AS ANTIPROLIFERATIVE AGENTS
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Page/Page column 69; 70; 72; 73, (2017/10/30)
The present invention refers to compounds of formula I or II endowed with DDX3 inhibitory activity, relative pharmaceutical compositions and their use as antihyperproliferative agents. (I) or (II)
HUMAN HELICASE DDX3 INHIBITORS AS THERAPEUTIC AGENTS
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Page/Page column 79; 80, (2016/09/22)
The present invention refers to compounds endowed with RNA helicase DDX3 inhibitory activity of formula I and II and their therapeutic use, in particular for the treatment of viral diseases.
Elaborate ligand-based pharmacophore exploration and QSAR analysis guide the synthesis of novel pyridinium-based potent β-secretase inhibitory leads
Al-Nadaf, Afaf,Sheikha, Ghassan Abu,Taha, Mutasem O.
experimental part, p. 3088 - 3115 (2010/07/08)
β-Secretase (BACE) inhibitors have potential as anti-Alzheimer's disease treatments prompting us to explore the pharmacophoric space of 129 known BACE inhibitors. QSAR analysis was employed to select optimal combination of pharmacophoric models and 2D physicochemical descriptors capable of explaining bioactivity variation (r2 = 0.88, F = 60.48, rLOO2 = 0.85, rPRESS2 against 25 external test inhibitors = 0.71). We were obliged to use ligand efficiency as the response variable because the logarithmic transformation of bioactivities failed to access self-consistent QSAR models. Three pharmacophoric models emerged in the successful QSAR equation suggesting at least three binding modes accessible to ligands within BACE binding pocket. QSAR equation and pharmacophoric models were validated through ROC curves and were employed to guide synthesis of novel pyridinium-based BACE inhibitors. The best inhibitor illustrated an IC50 value of 1.0 μM against BACE.
NOVEL ADENOSINE A3 RECEPTOR AGONISTS
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Page/Page column 72, (2008/06/13)
The invention realizes that a series of sulfonamido derivatives with a conserved uronamide group at the 5' position provide superior A3 receptor affinity as well as selectivity. These new adenosine agonists are sulfonamido deritatives N-substituted with aliphatic groups (cyclic or linear) or aromatic radicals.
