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Current studies included design, synthesis, and biological evaluations of 24 new compounds (series 3 6).
Most of the 4-hydroxy-3,5-dimethoxyphenyl biphenyl compounds (series II, 20 36) were in general more active than 3,4,5-trimethoxyphenyl biphenyl compounds (series I, 1 19).
Based on a definition of LC-HRMS signal series which can be caused by homologous compounds, series detection progresses in two stages.
Using 1400W [N- 3-aminomethylbenzyl)acetamidine], thiocitrulline and Nδ-(4,5-dihydrothiazol-2-yl)ornithine as lead compounds, series of N-benzyl- and N-phenyl-2-amino-4,5-dihydrothiazoles and thioureas were designed as inhibitors of NOS.
The g_ g conformers are found to be the most populated minima within the series of nonfluorinated compounds (series a), with significant amounts of pl conformers.
The compounds series was designed using a novel pharmacophore-based virtual screening approach, and notably the series could be fast and efficiently optimized using convergent MCR chemistry.
Similar(52)
Traditionally, SAR exploration has concentrated on individual compound series.
Compared to existing approaches these drawings substantially simplify the visual analysis of large compound series.
Changing substituent position revealed a more promising compound series of anti-inflammatory agents.
A long incubation time (e.g., 30 min) is more applicable to a compound series with high metabolic stability.
Additionally, data also suggest that increasing the bulk around C6 may allow control of subtype selectivity within these compound series.
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