inhibition of CYP3A4 activity may affect the metabolism of other co-administered drugs. Therefore, we screened for and developed a new class of boosters to improve the oral availability of drugs. We identified benzyloxyphenyl imidazole and phenethylphenyl imidazole derivatives as new types of CYP3A4 inhibitors. Among the compounds synthesized, an ester 5c was found to inhibit CYP activity and the compound
虽然细胞色素 P450 3A4 (CYP3A4)
抑制剂用作促进药物吸收以增加药物吸收,但抑制 CYP3A4 活性可能会影响其他共同给药药物的代谢。因此,我们筛选并开发了一类新的助推器,以提高药物的口服利用率。我们将苄氧基苯基
咪唑和苯
乙基苯基
咪唑衍
生物鉴定为新型 CYP3A4
抑制剂。在合成的化合物中,发现酯5c抑制CYP活性,并且化合物5c在生理条件下逐渐转化为无活性代谢物5d,表明酯5c可能代表一种新型的前药型增强剂。