Long-chain fatty dihydropyridines: Docking calcium channel studies and antihypertensive activity

• DOI: 10.1016/j.lfs.2020.118210
• Publication Date: 2020-08-05T01:30:29Z
• Authors: Eduarda Santa-Helena; Diego da Costa Ca...; Marcelo G. Montes...; João Luís Rheinga...; Matheus William B...; Adriano Velasque ...; Karina dos Santos...; Carla Amorim Neve...; Luiz Eduardo Maia...
• Keywords: Docking (animal)

From the synthesis of 43 lipophilic dihydropyridines, aim this study was to verify whether new dihydropyridines have calcium channel affinity using coupling studies and determine antihypertensive antioxidant properties, as well toxicology toxicity nifedipine three compounds, were chosen from previous results.The animals treated for 56 days, 28 days with N (ω) -nitro-L-arginine methyl ester induce hypertension, then another di- hydropyridine standard drug nifedipine. Throughout treatment had their blood pressure measured heart rate checked by pletysmography. After euthanised, samples collected creatine kinase urea analysis, brain, liver oxidative status analysis (quantification reactive oxygen species, total capacity, lipid peroxidation).Compounds 2c, 9a, significantly reduced control group levels. The tachycardia caused induction hypertension reversed 2c 9a compounds. Regarding stress analyzes, compounds that best performances also 9a. Overall results demonstrate two tested demonstrated performance equal or superior nifedipine.In study, first time, docking applied analyse fatty regarding binding. Afterwards, properties.