Beta-adrenergic blocking agents: substituted phenylalkanolamines. Effect of side-chain length on beta-blocking potency in vitro.
Beta-adrenergic blocking agents: substituted phenylalkanolamines. Effect of side-chain length on beta-blocking potency in vitro.
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β-肾上腺素能阻断剂：取代的苯基链烷醇胺。
DOI：
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发表时间：
1984
影响因子：
7.3
通讯作者：
H. Müller
中科院分区：
文献类型：
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作者：
W. Fuhrer;F. Ostermayer;M. Zimmermann;M. Meier;H. Müller
合成了一组在氮上带有新的5-乙氧基水杨酰胺取代基的潜在β-受体阻滞剂。测试这些化合物的体外β-肾上腺素能阻断效力，并与在氮上带有叔丁基的类似化合物进行比较。新的N-取代基大大增加了β-阻断效力。在Ar（CH 2）nCHOHCH 2NHR（R = 5-乙氧基水杨酰胺; n = 0-4）类型的一系列五种同源化合物中，发现n = 0和2时的两个最大β阻断效力。此外，相应的（芳氧基）丙醇胺的碳等排体仍然被证明是一种非常有效的β-受体阻滞剂。因此，侧链中的醚氧不是活性的绝对要求。结构-活性关系进行了讨论。
The synthesis of a group of potential beta-blockers bearing a new 5-ethoxysalicylamide substituent on nitrogen is described. These compounds were tested for beta-adrenergic blocking potency in vitro and compared with analogous compounds bearing a tert-butyl group on nitrogen. The new N-substituent increased the beta-blocking potency substantially. In a series of five homologous compounds of the type Ar(CH2)nCHOHCH2NHR (R = 5-ethoxysalicylamide; n = 0-4), two maxima of beta-blocking potency were found for n = 0 and 2. Moreover, the carbon isostere of the corresponding (aryloxy)propanolamine still proved to be a very potent beta-blocker. The ether oxygen in the side chain is therefore not an absolute requirement for activity. Structure-activity relationships are discussed.