超声与微波辅助合成及苯海拉明衍生物的抗糖尿病和造血活性

Ultrasound and Microwave-Assisted Synthesis and Antidiabetic and Hematopoietic Activity of Diphenhydramine Derivatives.

作者信息

Dauletbakov Anuar, Belyankova Yelizaveta, Assylbekova Saniya, Zolotareva Darya, Bayazit Sarah, Baktybayeva Layilya, Kemelbekov Ulan, Yu Valentina, Ibragimova Nailya, Zazybin Alexey

机构信息

School of Chemical Engineering, Kazakh-British Technical University, 59 Tole bi Str., Almaty 050000, Kazakhstan.

Department of Biophysics, Biomedicine and Neuroscience, Al-Farabi Kazakh National University, al-Farabi Ave, 71, Almaty 050040, Kazakhstan.

出版信息

Molecules. 2025 Jul 15;30(14):2967. doi: 10.3390/molecules30142967.

DOI:10.3390/molecules30142967

PMID:40733233

Abstract

This study presents the synthesis and antidiabetic and hematopoietic activity of ionic compounds based on 2-(diphenylmethoxy)-,-dimethylethanamine (diphenhydramine). Synthesis is carried out under ultrasonic (US) and microwave (MW) irradiation as well as using a conventional method (thermal activation). The synthesized ionic compounds have been tested for antidiabetic effect according to the inhibitory action against α-glucosidase and α-amylase (in vitro). All the synthesized derivatives of diphenhydramine showed higher inhibitory activity against α-glucosidase than commercially available diphenhydramine hydrochloride. Moreover, two of them, (66.9%) and (64.2%), had a greater inhibitory activity than the reference drug acarbose (51.8%). The hematopoietic activity was studied in albino laboratory female rats (in vivo). The compounds , , and can restore immune blood cells (hematopoietic activity), equal to or exceeding that of the commercially available diphenhydramine hydrochloride and control (methyluracil).

摘要

本研究介绍了基于2-(二苯基甲氧基)-N,N-二甲基乙胺（苯海拉明）的离子化合物的合成及其抗糖尿病和造血活性。合成是在超声（US）和微波（MW）辐射下以及使用传统方法（热活化）进行的。根据对α-葡萄糖苷酶和α-淀粉酶的抑制作用（体外）对合成的离子化合物进行了抗糖尿病作用测试。所有合成的苯海拉明衍生物对α-葡萄糖苷酶的抑制活性均高于市售盐酸苯海拉明。此外，其中两种化合物，（66.9%）和（64.2%），具有比参考药物阿卡波糖（51.8%）更高的抑制活性。在白化病实验雌性大鼠体内研究了造血活性。化合物、和可以恢复免疫血细胞（造血活性），等于或超过市售盐酸苯海拉明和对照（甲基尿嘧啶）。