RESUMO
Novel azole compounds were prepared which demonstrated potent hCB2 binding activities with antioxidant activity for a selected compound. These compounds show good selectivity over the hCB1 receptor and are full agonists at the hCB2 receptor.
Assuntos
Azóis/química , Azóis/metabolismo , Agonistas de Receptores de Canabinoides/química , Agonistas de Receptores de Canabinoides/metabolismo , Receptor CB2 de Canabinoide/agonistas , Receptor CB2 de Canabinoide/metabolismo , Animais , Células CHO , Canabinoides/química , Canabinoides/metabolismo , Cricetinae , Cricetulus , HumanosRESUMO
Novel phenolic thiazoles compounds were prepared which demonstrated potent antioxidant activity and potent in vivo neuroprotection in mitochondrial toxin models and also possess good oral bioavailability.
Assuntos
Antioxidantes/administração & dosagem , Fármacos Neuroprotetores/administração & dosagem , Fenóis/administração & dosagem , Tiazóis/administração & dosagem , Administração Oral , Animais , Antioxidantes/química , Relação Dose-Resposta a Droga , Intoxicação por MPTP/metabolismo , Intoxicação por MPTP/prevenção & controle , Camundongos , Fármacos Neuroprotetores/química , Fenóis/química , Substância Negra/efeitos dos fármacos , Substância Negra/metabolismo , Tiazóis/químicaRESUMO
The synthesis and biological activity of novel lipoic acid analogues are reported. Lipoic acid and structural homologues coupled to arylthiophene amidine via carboxamide linkers are metabolic antioxidants capable of protecting neuronal cells against glutamate cytotoxicity, preventing loss of intracellular glutathione, and inhibit nitric oxide synthase.
