Rational modification of a lead molecule: Improving the antifungal activity of indole – triazole – amino acid conjugates

Add time:07/16/2019    Source:sciencedirect.com

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.

We also recommend Trading Suppliers and Manufacturers of 3-(1H-indol-3-yl)aspartic acid (cas 83994-98-3). Pls Click Website Link as below: cas 83994-98-3 suppliers

Prev:Synthesis of 2,3,4,7-tetrahydro-1H-azepines as privileged ligand scaffolds for the design of aspartic protease inhibitors via a ring-closing metathesis approach
Next:Adsorption and competition investigation of phenolic compounds on the solid-liquid interface of three-dimensional foam-like graphene oxide)