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Structure guided design was used to optimize the series resulting in a significant potency improvement.
The results showed that most of the target compounds displayed significant potency to inhibit Aβ1 42 self-aggregation.
Introduction of an amide substituent at the 6-position of the pyridone core resulted in a significant potency increase.
In vitro studies showed that most of them exhibited significant potency to inhibit acetylcholinesterase and self-induced β-amyloid (Aβ) aggregation, and moderate antioxidant activity.
Five of these new conjugates were found to inhibit CHIKV in Vero cells with significant potency (EC50 = 10.2 19.1 μM) and showed low toxicity (CC50 = 75.2 178 μM).
Significant potency gains were observed with small aliphatic substituents such as methyl, n-propyl, and cyclopropyl when placed at the C-2 position of the chromane.
Similar(18)
SAR studies of the compounds performed for the four mouse GABA transporter proteins (mGAT1 mGAT4) implied significant potencies and subtype selectivities for 2-hydroxy-2-pyrrolidine-2-yl-acetic acid derivatives.
Inconsideration of its significant therapeutic potency, we conclude that TLJN has the potential, possibly as complementary and alternative therapy, to prevent and/or delay the deterioration of cognitive impairment in AD.
Potency of AMG 334 at the cyno CGRP receptor is similar to that at the human receptor, but with significant reduced potency at dog, rabbit and rat receptors.
More importantly, 5c exhibited significant neuroprotective potency against Aβ1-42-induced PC12 cell injury.
A majority of them displayed significant inhibitory potency and specific selectivity over PTP1B.
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