Sentence examples similar to a potent optimization from inspiring English sources

The tolyl triazole amides provided a potent platform amenable to optimization.

Design of a new core containing a cyclopropyl restriction yielded further PP improvements and when combined with the termini SAR optimizations yielded a potent and highly selective agonist suitable for further preclinical development (58).

NVP-BHG712 was synthesized based on rational design and further optimization led to a potent and selective inhibitor of the EphB4 receptor tyrosine kinase, as demonstrated in cell based assays.

Optimization of the dihydropyrone series afforded a potent antiviral agent, PD 178390 (EC50=0.20 μM, TD50=>100 μM).

Hence, core crystallinity was found to be a potent tool for tailoring micelle properties and thereby facilitating the optimization of drug delivery systems.

Optimization leads to the identification of compound 3c, a potent and orally available agent with improved physicochemical and pharmacokinetic properties.

Optimization of this series led to the identification of a potent and selective PPARδ agonist 17.

Optimization of derivative 23 resulted in the design of a potent dicarboxamide 47, which displayed a Ki of 135 nM.

Based on our previous study with trifluoroethylamine as a P2-P3 amisosteretere of cathepsin K inhibitor, further optimization led to identification of compound 22 (L-873724) as a potent and selective non-basic cathepsin K inhibitor.

After two rounds of optimizations, the compound I-14 was found to be a potent proteasome inhibitor.

A potent and selective inhibitor of Akt1 and Akt2 (AKTi-1/2; naphthyridinone) was prepared through optimization of leads identified by a high-throughput screen for inhibitors of purified activated Akt1, Akt2 and Akt3 kinases [21].