Studies on Propafenone??type Modulators of Multidrug??Resistance IV: Synthesis and Pharmacological Activity of 5??Hydroxy and 5??Benzyloxy Derivatives

P Chiba, B Tell, W Jäger, E Richter…

文献索引：Chiba, Peter; Tell, Barbara; Jaeger, Walter; Richter, Elisabeth; Hitzler, Manuela; Ecker, Gerhard Archiv der Pharmazie, 1997 , vol. 330, # 11 p. 343 - 347

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被引用次数: 22

摘要

Abstract A series of 5-hydroxy and 5-benzyloxy analogs of the antiarrhythmic and multidrug resistance (MDR) modulating drug propafenone was synthesized and the MDR-modulating activity of the compounds was evaluated using a daunomycin efflux assay system. The key step of the synthesis is the selective reduction of the double bond in 1 without cleavage of the benzyl group thus leading to the phenol 3. Alkylation with epichlorohydrine followed ...