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用Hansch途径研究了一系列3-甲基芬太尼衍生物理化性质与镇痛活性间的关系。初步结果表明,镇痛活性与化合物的油/水分配系数之间无规律性变化;与R_2取代基的立体效应(如L,B_1～B_4及MR_(R2))和疏水常数(π_(R2))间有一定的匹配关系,与R_3取代基的Hammen常数(σ)呈抛物线型。引入1-β羟基亦颇为有利。从作用机理推测,该类衍生物的R_2和■可能是与受体相结合的基团,R_1可能仅起药物转运的载体作用,1-β羟基也可能通过氢键参与与受体的互补部位缔合。
The relationship between physico-chemical properties and analgesic activities of a series of 3-methylfentanyl derivatives was investigated using the Hansch pathway. The preliminary results showed that there was no regular change between the analgesic activity and the oil / water partition coefficient of the compound; the stereoscopic effect (such as L, B_1 ~ B_4 and MR_ (R2)) and the hydrophobic constant (π_ (R2) ), And the Hammen constant (σ) of R_3 substituent is parabolic. It is also advantageous to introduce 1-beta hydroxyl groups. It is speculated from the mechanism of action that R 2 and R 2 of these derivatives may be groups that bind to the receptor. R 1 may only act as a carrier for drug transport. The 1-β hydroxyl may also participate in the site complementary to the receptor Associate