A new class of shape-modified nucleosides is introduced. These novel "fleximers" feature the purine ring systems of adenosine, inosine, and guanosine split into their individual imidazole and pyrimidine components (as in 1-3). This structural modification serves to introduce flexibility into the nucleoside while still retaining the elements essential for recognition. As a consequence, these novel fleximers should find use as bioprobes for investigating enzyme-coenzyme binding sites as well as nucleic acid and protein interactions. Their design and synthesis are described.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/jo0255476 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Drug Development.
Alzheimers Dement
December 2024
Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Patiala, India.
Background: Neuroinflammation plays an important role in progression of Alzheimer's disease (AD). Interlukin-6 (IL-6) is well identified marker in initiating and regulating inflammation, and formation of senile plaques in brain. Therefore, simultaneous inhibition of both IL-6 and acetylcholinesterase (AChE) may be an effective strategy for AD.
View Article and Find Full Text PDFDrug Development.
Alzheimers Dement
December 2024
Indiana University School of Medicine, Indianapolis, IN, USA.
Background: The TREAT-AD centers aim to improve Alzheimer's Disease (AD) research by offering free, high-quality tools and technologies. Lyn is a tyrosine kinase that belongs to the Src family kinases. The expression of Lyn and its activity have been implicated in AD.
View Article and Find Full Text PDFDrug Development.
Alzheimers Dement
December 2024
Merry Life Biomedical Company, Ltd., Tainan City, Taiwan, Taiwan.
Background: Alzheimer's disease (AD) is complex in pathogenesis and related to aging biology, especially in late-onset AD. We identified a novel synthetic curcumin analog TML-6 through the platform of 6 biomarkers of anti-aging, anti-inflammation, and anti-Aβ as the potential AD drug candidate. TML-6 exhibits multi-target effects on AD pathogenesis, including the activation of NrF-2, the regulation of autophagic machinery through mTOR, the inhibition of APP synthesis and reduction of Aβ, the upregulation of ApoE, and the inhibition of microglial activation.
View Article and Find Full Text PDFDrug Development.
Alzheimers Dement
December 2024
Burke Neurological Institute, Weill Cornell Medicine, White Plains, NY, USA.
Background: Benfotiamine, a prodrug of thiamine, raises blood levels by 50-100 times to achieve pharmacologic effects. It provides a novel therapeutic direction addressing a well-characterized brain tissue thiamine deficiency and related changes in glucose metabolism in AD. BenfoTeam is a seamless phase 2A-2B "proof of concept" (POC), double-blind, placebo-controlled RCT investigating tolerability, safety, and efficacy of benfotiamine, as a first-in-class small molecule treatment for early AD.
View Article and Find Full Text PDFBackground: The present study demonstrates the design, synthesis and pharmacological evaluation of coumarin-oxadiazole hybrids as potential molecules of therapeutic significance for the treatment of cognitive dysfunction.
Method: Eight novel coumarin-oxadiazole hybrids have been synthesized by employing suitable synthetic procedures and characterized by various spectral techniques i.e.
Want 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!