Design, Synthesis and Biological Evaluation of Lophanic Acid Derivatives as Antifungal and Antibacterial Agents.
Molecules
; 27(20)2022 Oct 12.
Article
in En
| MEDLINE
| ID: mdl-36296430
ABSTRACT
In order to discover more promising antifungal and antibacterial agents, a series of new derivatives were designed and synthesized by structure modification based on the naturally occurring antimicrobial compound lophanic acid. The structures of all the target compounds were well characterized by spectroscopic data. The stereochemistry of these compounds was further determined through the X-ray diffraction analysis of 6a. The synthetic compounds were evaluated for their antimicrobial activities against filamentous fungi (T. rubrum, T. mentagrophytes), yeasts (C. neoformans, C. albicans) and Gram-positive and Gram-negative bacteria (MRSA, S. mutans, S. sobrinus, and E. coli). Among them, 3d and 3i are found as the most promising leads that showed potent inhibitory effects against all the tested fungal and bacterial strains except for E. coli. The presence of the C-20 carboxylic ester groups and the free hydroxy group at C-13 was found to be essential for the antifungal and antibacterial activities of the lophanic acid derivatives.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Anti-Infective Agents
/
Antifungal Agents
Language:
En
Journal:
Molecules
Journal subject:
BIOLOGIA
Year:
2022
Document type:
Article
Affiliation country:
China
Publication country:
CH
/
SUIZA
/
SUÍÇA
/
SWITZERLAND