The SAR results imply that lipophilic effect of dimethoxy groups
(R1) enhances the activity of triazoles type I and type III. Our results
are in-line with earlier studies, in which the lipophilicity is responsible
for high aromatase inhibition of xanthone10 and coumarin11
derivatives. Even with or without dimethoxy groups, the triazoles
type II with restricted THIQ were shown to be inactive compounds.
This could be possibly due to their structural features, that is, flexible
or rigid conformation, isomeric effect and binding interaction
with the target site of action. Therefore, the aid of molecular docking
may provide insight into their mechanism of action.
The SAR results imply that lipophilic effect of dimethoxy groups(R1) enhances the activity of triazoles type I and type III. Our resultsare in-line with earlier studies, in which the lipophilicity is responsiblefor high aromatase inhibition of xanthone10 and coumarin11derivatives. Even with or without dimethoxy groups, the triazolestype II with restricted THIQ were shown to be inactive compounds.This could be possibly due to their structural features, that is, flexibleor rigid conformation, isomeric effect and binding interactionwith the target site of action. Therefore, the aid of molecular dockingmay provide insight into their mechanism of action.
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