I found the field of Pharmacology & Pharmacy very interesting. Saw the article Effects of steric hindrance and electron density of ester prodrugs on controlling the metabolic activation by human carboxylesterase published in 2021.0. Formula: C8H8O2, Reprint Addresses Takahashi, M (corresponding author), Chiba Inst Sci, Fac Pharm, 15-8 Shiomi Cho, Choshi, Chiba 2880025, Japan.. The CAS is 99-93-4. Through research, I have a further understanding and discovery of 4′-Hydroxyacetophenone
Carboxylesterase (CES) plays an important role in the hydrolysis metabolism of ester-type drugs and prodrugs. In this study, we investigated the change in the hydrolysis rate of hCE1 by focusing on the steric hindrance of the ester structure and the electron density. For 26 kinds of synthesized indomethacin prodrugs, the hydrolytic rate was measured in the presence of human liver microsomes (HLM), human small intestine microsomes (HIM), hCE1 and hCE2. The synthesized prodrugs were classified into three types: an alkyl ester type that is specifically metabolized by hCE1, a phenyl ester type that is more easily metabolized by hCE1 than by hCE2, and a carbonate ester type that is easily metabolized by both hCE1 and hCE2. The hydrolytic rate of 1-methylpentyl (hexan-2-yl) ester was 10-times lower than that of 4-methylpentyl ester in hCE1 solution. hCE2 was susceptible to electron density of the substrate, and there was a difference in the hydrolysis rate of up to 3.5-times between p-bromophenyl ester and p-acetylphenyl ester. By changing the steric hindrance and electron density of the alkoxy group, the factors that change the hydrolysis rate by CES were elucidated. (C) 2021 The Japanese Society for the Study of Xenobiotics. Published by Elsevier Ltd. All rights reserved.
Formula: C8H8O2. Bye, fridends, I hope you can learn more about C8H8O2, If you have any questions, you can browse other blog as well. See you lster.
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles