Several multifunctional benzothiadiazine derivatives were synthesized and examined for their inhibition to the enzyme aldose reductase and in vitro antioxidant activity to identify novel drugs for diabetes and its complications. Most of them exhibited good inhibitory activity. Importantly, a number of compounds demonstrated strong antioxidant activity and one compound in particular was extremely active in the DPPH radical scavenging and MDA inhibition analysis. The DPPH radical scavenging rate with this compound was 98.0%, 92.3% and 42.1% at concentrations of 100μM, 10μM, and 1μM, respectively, and the initial reaction rate was faster than Trolox at a concentration of 10μM.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2016.04.047 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
CD73: agent development potential and its application in diabetes and atherosclerosis.
Front Immunol
December 2024
The Affiliated Hospital of Qingdao University, Qingdao University, Qingdao Cancer Institute, Qingdao, Shandong, China.
CD73, an important metabolic and immune escape-promoting gene, catalyzes the hydrolysis of adenosine monophosphate (AMP) to adenosine (ADO). AMP has anti-inflammatory and vascular relaxant properties, while ADO has a strong immunosuppressive effect, suggesting that CD73 has pro-inflammatory and immune escape effects. However, CD73 also decreased proinflammatory reaction, suggesting that CD73 has a positive side to the body.
View Article and Find Full Text PDFArticle Synopsis
- A four-year-old girl experienced persistent hypoglycemia shortly after birth and was diagnosed with congenital hyperinsulinism due to genetic mutations in the ABCC8 gene.
- She did not respond to typical treatments like oral diazoxide but showed improvement with subcutaneous somatostatin injections.
- At age three and a half, her treatment was changed to a long-acting somatostatin analogue, leading to better blood sugar control, normal growth, and the ability to stop tube feeding.
Synthesis of N-heterocyclic compounds using ,-dimethylacetamides as an electrophilic carbon source.
Org Biomol Chem
November 2024
Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul, 08826, Republic of Korea.
In this study, N-heterocyclic compounds were synthesized using nitrogen-containing nucleophilic substrates and electrophilic carbon sources derived from ,-dimethylacetamide (DMAc). Depending on the nucleophilic groups, N-heterocyclic compounds such as 4-quinazolinones, pyrrole-quinoxalines, and dihydro-benzothiadiazine dioxides were produced. Carbon, adjacent to the nitrogen in DMAc, was activated in the presence of FeCl·6HO and di--butyl peroxide (DTBP).
View Article and Find Full Text PDFA Refined Thin-Film Model for Drug Dissolution Considering Radial Diffusion - Simulating Powder Dissolution.
Pharm Res
May 2024
Synthetic Molecule Pharmaceutical Sciences, Genentech, Inc., 1 DNA Way, South San Francisco, CA, 94080, USA.
Purpose: We aim to present a refined thin-film model describing the drug particle dissolution considering radial diffusion in spherical boundary layer, and to demonstrate the ability of the model to describe the dissolution behavior of bulk drug powders.
Methods: The dissolution model introduced in this study was refined from a radial diffusion-based model previously published by our laboratory (So et al. in Pharm Res.
Evaluation of the translation of multiple cardiovascular regulatory mechanisms in the anesthetized dog.
J Pharmacol Toxicol Methods
March 2024
AbbVie Inc., 1 North Waukegan Rd., North Chicago, IL 60064, United States of America.
The strategic and targeted use of an anesthetized canine cardiovascular model early in drug discovery enables a comprehensive cardiovascular and electrophysiological assessment of potential safety liabilities and guides compound selection prior to initiation of chronic toxicological studies. An ideal model would enable exposure-response relationships to guide safety margin calculations, have a low threshold to initiate, and have quick delivery of decision quality data. We have aimed to profile compounds with diverse mechanism of actions (MoAs) of "non-QT" cardiovascular drug effects and evaluate the ability of nonclinical in vivo cardiovascular models to detect clinically reported effects.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!