Synthesis of drimanyl indole fragments of drimentine alkaloids and their antibacterial activities.

Bioorg Med Chem Lett

College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, Shaanxi, China. Electronic address:

Published: February 2025

Two types of drimanyl indole fragments of drimentine alkaloids were synthesized and evaluated their in vitro antibacterial activities using minimum inhibitory concentration. Analysis of structure-activity relationship against Ralstonia solanacearum revealed that fragment I exhibited superior inhibitory activity compared to fragment II. Notably, free NH of the indole motif was essential for antibacterial activity, while COH of the drimane skeleton was beneficial for enhancing the inhibitory effect. Compound 2, possessing these structural features, showed the highest activity to R. solanacearum among all the tested compounds with a MIC value of 8 µg/mL, indicating its potential as a promising lead for the development of novel antibiotics.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2024.130040DOI Listing

Publication Analysis

Top Keywords

drimanyl indole
8
indole fragments
8
fragments drimentine
8
drimentine alkaloids
8
antibacterial activities
8
synthesis drimanyl
4
alkaloids antibacterial
4
activities types
4
types drimanyl
4
alkaloids synthesized
4

Similar Publications

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!