A new class of cardiotonic agents: structure-activity correlations for natural and synthetic analogs of the alkaloid pumiliotoxin B (8-hydroxy-8-methyl-6-alkylidene-1- …

…, ET McNeal, LE Overman, DH Ellison

文献索引：Daly; McNeal; Overman; Ellison Journal of Medicinal Chemistry, 1985 , vol. 28, # 4 p. 482 - 486

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被引用次数: 30

摘要

Pumiliotoxin B (PTX-B, 6-(6', 7'-dihydroxy-2', 5'-dimethyl-(E)-4'-octenylidene)-8-hydroxy-8- methyl-l-azabicyclo-[4.3. 0] nonane) increases the force of contractures of spontaneously beating guinea pig atrial strips by 3-to &fold with half-maximal effects at about 3 pM and increases rates of atrial contractions by 2-to% fold with half-maximal effects at about 6 pM. The presence of an axial 7-hydroxy substituent (PTX 339A) decreases the efficacy but not ...