Browsing by Author "Chung, Hery"
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- Item2D-QSAR and 3D-QSAR/CoMSIA Studies on a Series of (R)-2-((2-(1H-Indol-2-yl)ethyl)amino)-1-Phenylethan-1-ol with Human β₃-Adrenergic Activity(2017) Apablaza H., Gastón E.; Montoya, Luisa; Morales Verdejo, César Aarón; Mellado, Marco; Cuellar Fritis, Mauricio Alcides; Lagos, Carlos F.; Soto Delgado, Jorge; Chung, Hery; Pessoa Mahana, Carlos David; Jaime Mella
- ItemCannabidiol binding and negative allosteric modulation at the cannabinoid type 1 receptor in the presence of delta-9-tetrahydrocannabinol: an In Silico study(2019) Chung, Hery; Fierro Huerta, Angélica; Pessoa Mahana, Carlos David
- ItemNew Pyridone-Based Derivatives as Cannabinoid Receptor Type 2 Agonists(MDPI, 2021) Faundez Parraguez, Manuel; Alarcon Miranda, Carlos; Cho, Young Hwa; Pessoa Mahana, Hernan; Gallardo Garrido, Carlos; Chung, Hery; Faundez, Mario; Pessoa Mahana, DavidThe activation of the human cannabinoid receptor type II (CB2R) is known to mediate analgesic and anti-inflammatory processes without the central adverse effects related to cannabinoid receptor type I (CB1R). In this work we describe the synthesis and evaluation of a novel series of N-aryl-2-pyridone-3-carboxamide derivatives tested as human cannabinoid receptor type II (CB2R) agonists. Different cycloalkanes linked to the N-aryl pyridone by an amide group displayed CB2R agonist activity as determined by intracellular [cAMP] levels. The most promising compound 8d exhibited a non-toxic profile and similar potency (EC50 = 112 nM) to endogenous agonists Anandamide (AEA) and 2-Arachidonoylglycerol (2-AG) providing new information for the development of small molecules activating CB2R. Molecular docking studies showed a binding pose consistent with two structurally different agonists WIN-55212-2 and AM12033 and suggested structural requirements on the pyridone substituents that can satisfy the orthosteric pocket and induce an agonist response. Our results provide additional evidence to support the 2-pyridone ring as a suitable scaffold for the design of CB2R agonists and represent a starting point for further optimization and development of novel compounds for the treatment of pain and inflammation.
- ItemSynthesis and docking of novel 3-indolylpropyl derivatives as new polypharmacological agents displaying affinity for 5-HT1AR/SERT(2016) Pessoa Mahana, Hernán; Silva Matus, Paul; Pessoa Mahana, Carlos David; Chung, Hery; Iturriaga Vásquez, Patricio; Quiroz, Gabriel; Möller Acuña, Patricia; Zapata Torres, Gerald; Saitz Barría, Claudio Antonio; Araya Maturana, Ramiro; Reyes Parada, Miguel
- ItemSynthesis, in vitro evaluation and molecular docking of a new class of indolylpropyl benzamidopiperazines as dual AChE and SERT ligands for Alzheimer's disease(2020) Rodríguez Lavado, J.; Gallardo Garrido, C.; Mallea, M.; Bustos, V.; Osorio, R.; Hodar Salazar, M.; Chung, Hery; Araya Maturana, Ramiro; Lorca, M.; Pessoa Mahana, Carlos David; Mella Raipán, Jaime Alberto; Saitz Barría, Claudio Antonio; Jaque Olmedo, Pablo César; Reyes Parada, M.; Iturriaga Vásquez, P.; Pessoa Mahana, Hernán