Category Ranking
98%
Total Visits
921
Avg Visit Duration
2 minutes
Citations
20
Article Abstract
Herein, we present two 17(15→16)--abietane diterpenoids ( and ) as the first terpenoid-class Na1.8 inhibitors, along with their first asymmetric total syntheses to enable in-depth pharmacological studies. Key steps include kinetic resolution of terminal epoxides, bioinspired polyene cyclization, and late-stage photocatalytic benzylic oxidation. Preliminary structural modifications led to 13 derivatives, among which compound exhibited both a 4.3-fold improved potency compared to parent natural product and preserved selectivity across other sodium-gated sodium channels.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/acs.orglett.5c02746 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Asymmetric Total Synthesis of (+)-Spiroapplanatumine G.
Org Lett
September 2025
School of Chemical Sciences, University of Auckland, 23 Symonds Street, Auckland 1010, New Zealand.
Spiroapplanatumine G () is a spiro-meroterpenoid characterized by an unusual 6/5/7 tricyclic spirobenzofuran-3-one core. The first enantioselective total synthesis of spiroapplanatumine G () is reported, featuring a key enantioselective Diels-Alder reaction between an aurone ester and a silyloxydiene to assemble the spirobenzofuranone core. This strategic Diels-Alder transformation advantageously establishes the two contiguous stereogenic centers in a single step.
View Article and Find Full Text PDFSynthesis of ()- and ()-4-Hydroxy-2-cyclopenten-1-ones: Total Synthesis of Entecavir, Abacavir, and Carbovir.
J Org Chem
September 2025
School of Pharmaceutical Sciences, Nanjing Tech University, 30 South Puzhu Road, Nanjing 211816, China.
A new synthetic procedure was developed for the chiral synthons ()- and ()- that enabled us to complete the asymmetric total synthesis of entecavir, abacavir, and carbovir. This lipase-based procedure holds good potential for developing a green process for the industrial production of ()- and ()- with a high enantiomeric purity. The asymmetric synthesis of entecavir was powered by the highly challenging Michael addition-elimination reaction.
View Article and Find Full Text PDFAim: This study aims to investigate the difference in C1 laminectomy length between the right and left sides and to determine the importance of considering the dominant vertebral artery in reducing complication risks.
Material And Methods: A total of five caucasian male cadavers were studied. The distance of the C1 posterior tubercle to the vertebral groove (A), the length of the vertebral groove (B) and diameter of vertebral artery were measured and statistically investigated.
Stereoselective convergent total synthesis of tonkinelins.
Org Biomol Chem
September 2025
Department of Chemistry, Indian Institute of Technology Bombay, Powai, Mumbai 400076, Maharashtra, India.
We report the stereoselective synthesis of (17,18,36)-tonkinelin and its diastereomer (17,18,36)-tonkinelin a convergent strategy involving the stepwise construction of two key fragments: a chiral ester-derived phosphonium salt and a requisite aldehyde for a convergent Wittig olefination. Key transformations in the sequence include asymmetric dihydroxylation, Wittig olefination, ring-closing metathesis (RCM) and chemoselective diimide olefin reduction. The synthesized tonkinelins were fully characterized, and their spectroscopic data were found to be consistent with previously reported data.
View Article and Find Full Text PDFRadiostereometric Insights into Total Knee Arthroplasty: Cemented and Uncemented Fixation with an Asymmetrical Tibial Component: Commentary on an article by Müjgan Yilmaz Altun, BPT, MD, PhD, et al.: "Migration of Cemented and Uncemented Implants in Total Knee Arthroplasty with an Asymmetrical Tibial Component. A Randomized Controlled Trial with a 2-Year Model-Based Radiostereometric Analysis Follow-up".
J Bone Joint Surg Am
September 2025
Department of Orthopaedic Surgery and Sports Medicine, University of Washington School of Medicine, Seattle, Washington.