Synthesis and pharmacological evaluation of 1-alkyl-N-[2-ethyl-2-(4-fluorophenyl) butyl] piperidine-4-carboxamide derivatives as novel antihypertensive agents

S Watanuki, K Matsuura, Y Tomura, M Okada…

文献索引：Watanuki, Susumu; Matsuura, Keisuke; Tomura, Yuichi; Okada, Minoru; Okazaki, Toshio; Ohta, Mitsuaki; Tsukamoto, Shin-Ichi Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 18 p. 5628 - 5638

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被引用次数: 6

摘要

We synthesized and evaluated inhibitory activity against T-type Ca2+ channels for a series of 1-alkyl-N-[2-ethyl-2-(4-fluorophenyl) butyl] piperidine-4-carboxamide derivatives. Structure–activity relationship studies have revealed that dialkyl substituents at the benzylic position play an important role in increasing inhibitory activity. Oral administration of N-[2- ethyl-2-(4-fluorophenyl) butyl]-1-(2-phenylethyl) piperidine-4-carboxamide (20d) lowered ...