Optimization of Compound

Superimposition of 3 and 4, as shown in Fig. 4, showed that the phenyl rings on the left side occupied different positions in space. If both compounds were accepted by the enzsmie, it followed that both positions should have been possible simultaneously. It was therefore imme- 

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Drug discovery is the identification and optimization of compounds for further development of drugs. 

Numerous highly potent and selective substance P antagonists are known, some of which were obtained from optimization of compounds identified during random screening.In addition, Hirschmann et al.i47 found excellent antagonist activity at the SP receptor (IC50 = 60 nM) with a (3-D-glucose-based peptidomimetic. 

Fluorine can also be used as a bioisosteric replacement of hydrogen to reduce clearance, not by blocking oxidative metabolism directly, but by reducing electron density from metaboUcally soft positions. This strategy has been applied in the optimization of compounds directed at Alzheimer s disease (Figure 3.16). Linopir-dine is a compound that enhances potassium-evoked release of acetylcholine, but was... 

The optimization of compounding technologies and installations aim now to establish the optimum blend composition, depending on the required blend and components characteristics, to choose the most suitable compounding equipment and its operating... 

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