Synthesis and preliminary biological evaluation of resveratrol-like carbostyril derivatives as sirtuin 1 modulators and cyclooxygenase inhibitors.

Authors

Toshihiko Tashima, Yoshinori Suzuma, Hiroaki Murata, Hidehiko Kodama

Published in

Bioorganic & medicinal chemistry letters. Pages 130741. Jul 25, 2026. Epub Jul 25, 2026.

Abstract

Resveratrol is an antioxidant polyphenolic compound found in grape skins and red wine. It has been suggested that resveratrol mediates sirtuin 1 (SIRT1) activation, leading to anti-aging, life extension, and anti-cancer effects as demonstrated primarily in model organisms. Additionally, resveratrol inhibits cyclooxygenase-2 (COX-2), resulting in anti-inflammatory effects in atopic dermatitis and psoriasis as well as suppression of carcinogenesis. Thus, resveratrol is a pharmacologically multifunctional compound. However, it suffers from low oral bioavailability and a short half-life. Carbostyril (2-quinolinone, 2-quinolone) has been adopted as a structural scaffold in natural products as well as in pharmaceutical agents and physiologically active substances. The carbostyril scaffold is recognized for its biological stability and lack of toxicity. Consequently, replacing parts of lead or model compounds with carbostyril scaffolds as bioisosteres may generate promising pharmaceutical agents with reduced toxicity. In this study, we synthesized and biologically evaluated resveratrol-like carbostyril derivatives as SIRT1 modulators or COX inhibitors.

PMID:
42501763
Bibliographic data and abstract were imported from PubMed on 26 Jul 2026.

Read full publication at:
Please sign in to see all details.

Stats

1-terrible, 9-excellent. How would you rate this publication? Sign in in to submit your rating.

Post a comment

You need to be signed in to post comments. You can sign in here.

Comments

There are no comments yet.