Synthesis, evaluation, and docking study of adamantyl-1,3,4-oxadiazol hybrid compounds as CaMKIIδ kinase inhibitor

Author:

Al-Mahadeen Mohammed M1,Jaber Areej M2ORCID,Al-Qawasmeh Raed A13,Taha Mutasem O4

Affiliation:

1. Department of Chemistry, Faculty of Science, The University of Jordan, Amman, Jordan

2. Pharmacological and Diagnostic Research Center, Faculty of Pharmacy, Al-Ahliyya Amman University, Amman, Jordan

3. Pure and Applied Chemistry Group, Department of Chemistry, College of Sciences, University of Sharjah, Sharjah, UAE

4. Drug Discovery Unit, Faculty of Pharmacy, The University of Jordan, Amman, Jordan

Abstract

This study revealed a new inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII), a crucial factor in cardiovascular disease and hypertension. The study focuses on the bioactivity compounds that combine adamantane/1,3,4-oxadiazole, potentially inhibiting CaMKIIδ. Various adamantyl-1,3,4-oxadiazole derivatives were synthesized and tested for their efficiency against CaMKIIδ kinase, with 6f being the most potent with an IC50 value of 14.4 μM. Docking studies were carried out to determine the binding processes of these chemicals within the kinase’s active region. These discoveries are an important step toward the development of novel treatments for cardiovascular illnesses and hypertension, with the potential for more precise and efficient therapeutic interventions in the future.

Publisher

SAGE Publications

同舟云学术

1.学者识别学者识别

2.学术分析学术分析

3.人才评估人才评估

"同舟云学术"是以全球学者为主线,采集、加工和组织学术论文而形成的新型学术文献查询和分析系统,可以对全球学者进行文献检索和人才价值评估。用户可以通过关注某些学科领域的顶尖人物而持续追踪该领域的学科进展和研究前沿。经过近期的数据扩容,当前同舟云学术共收录了国内外主流学术期刊6万余种,收集的期刊论文及会议论文总量共计约1.5亿篇,并以每天添加12000余篇中外论文的速度递增。我们也可以为用户提供个性化、定制化的学者数据。欢迎来电咨询!咨询电话:010-8811{复制后删除}0370

www.globalauthorid.com

TOP

Copyright © 2019-2024 北京同舟云网络信息技术有限公司
京公网安备11010802033243号  京ICP备18003416号-3