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To optimize the potency of the ECT, a balance between adequate anesthesia and optimal duration of induced seizure is crucial.
Here, we applied multiple approaches to optimize the potency and selectivity of our reported alloxazine scaffold.
Topliss operational method was used to optimize the potency of molecules.
Further synthetic modification was undertaken to optimize the potency of amide compounds.
Information from X-ray crystal structures were used to optimize the potency of a HTS hit in a Hsp90 competitive binding assay.
In our desire to optimize the potency of 5, compounds 6 (3ξ-fluoro) and 9 (3β-sulfamate) designed to increase the stability and oral bioavailability of 5, respectively were evaluated in vivo.
Similar(49)
The present study was directed at optimizing the potency of SIRT2 inhibitors containing the neuroprotective sulfobenzoic acid scaffold and improving their pharmacology.
Structure-based design aided in optimizing the potency of the initial lead (2, IC50 of 11 μM) to a potent (11l, 190 nM) EGLN-1 inhibitor.
Molecular variations involving the study of homologous series or the application of the vinylogy concept induce relatively minor changes of the pharmacological profile and result in optimizing the potency.
Chemical modifications can optimize the inotropic potency of APLs opening a novel field of therapeutic opportunities.
In order to optimize the inhibitory potency, a binding model for PCAF inhibition by anacardic acid was proposed and new anacardic acid derivatives were designed.
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