Exact(60)
Most compounds showed moderate to excellent potency.
The 4-hydroxy derivatives showed excellent potency and selectivity.
Compound 33 exhibited excellent potency, selectivity over A1, and reduced hERG liability.
The results revealed that most compounds possessed moderate to excellent potency.
These studies resulted in the identification of several compounds which showed excellent potency against PAI-1.
In particular, compounds 52 54 showed excellent potency against cancer cells.
Compound (S -4g S -4gd excellent potency with IC50 of 20 nM for BACE1.
Tricyclic sulfones were designed as γ-secretase inhibitors and found to have excellent potency.
The resulting ketones demonstrated excellent potency and selectivity for fXa but initially had poor oral bioavailability.
This series exhibits excellent potency against key yeast and dermatophyte strains.
In a similar study, two novel derivatives of THIQ (Fig. 2a and b) showed excellent potency against wild strains of HIV-1 by inhibiting RT enzyme [13].
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