Kumar Atul, Maurya Ram Awatar, Sharma Siddharth
Medicinal and Process Chemistry Division, Central Drug Research Institute(dagger), Lucknow 226001, India.
Bioorg Med Chem Lett. 2009 Aug 1;19(15):4432-6. doi: 10.1016/j.bmcl.2009.05.056. Epub 2009 May 19.
Human hemoglobin (HbA) efficiently catalyses the oxidative aromatization of 1,4-dihydropyridines (1,4-DHPs) and pyrazolines with hydrogen peroxide in phosphate buffer. The results of the study reveal that the rates of oxidative aromatization of 1,4-DHPs are substituent dependent. Thus, the present study is very useful in understanding the metabolism of 1,4-DHP drugs in liver by cytochrome P450 and designing novel drugs as well as modifying the existing drugs for better pharmacokinetic profile.
人血红蛋白(HbA)在磷酸盐缓冲液中能有效催化1,4 - 二氢吡啶(1,4 - DHPs)和吡唑啉用过氧化氢进行氧化芳构化反应。研究结果表明,1,4 - DHPs的氧化芳构化速率取决于取代基。因此,本研究对于理解细胞色素P450在肝脏中对1,4 - DHP药物的代谢、设计新型药物以及改进现有药物以获得更好的药代动力学特性非常有用。