Basic Information
ID: ALA4152315
Journal: Eur J Med Chem
Title: Rational modification of a lead molecule: Improving the antifungal activity of indole - triazole - amino acid conjugates.
Authors: Mishra S, Kaur M, Chander S, Murugesan S, Nim L, Arora DS, Singh P.
Abstract: The modification of a molecule that was identified as highly efficacious in the previous studies could considerably improve the biological activity of the resulting compounds. While targeting lanosterol 14-α demethylase, the molecular modelling studies convinced that the extension of the phenyl ring of compound 1 deep into the hydrophobic pocket of the enzyme may increase the enzyme - ligand interactions and hence improve the anti-fungal profile of the molecules. As a result, the newly designed compounds 2 were synthesized and screened for their anti-microbial properties and these compounds were found to exhibit considerably better activity than the previous molecule 1. Some of the compounds in this series exhibited MIC90 16 μg mL-1 and 32 μg mL-1 against Candida albicans and Aspergillus niger, respectively as against 312 μg mL-1 for compound 1.
CiteXplore: 29936353
DOI: 10.1016/j.ejmech.2018.06.039
Patent ID: ┄
Associated Items: Associated Bioactivities Associated Assays Associated Compounds Associated Targets