Al'tshuler R A, Parshin V A
Farmakol Toksikol. 1980 Mar-Apr;43(2):153-8.
It was shown in experiments on mice and rats that increased hydrophobic properties of the phenylcarbomoyl radical to sydnocarb attained by introduction of halogens of trifluoromethylene in the benzene ring is conducive to the production of compounds that are similar to sydnocarb by the spectrum of the central stimulant action but are 2--4 times more active. In contradistinction to phenamine and its analogues the replacement of beta-phenylisopropyl chain by beta-phenylethyl one is not followed by an abrupt decrease in the activity in the series of compounds tested.
在对小鼠和大鼠的实验中表明,通过在苯环中引入三氟亚甲基卤素,使苯基甲酰基对西地那非的疏水性增加,有利于产生与西地那非具有相似中枢兴奋作用谱但活性高2至4倍的化合物。与苯乙胺及其类似物不同,在测试的一系列化合物中,用β-苯乙基取代β-苯异丙基链后,活性不会突然降低。