Scaffolding general

The simplest synthetic approach to the preparation of monofunctional dendritic systems is to functionalise the periphery of existing molecular scaffolds, generally constructed by divergent or convergent growth (Fig. 3.2, Route a) or b), respectively). 

Although the traditional steroidal agonists and nonsteroidal antagonists are used for a narrow spectrum of diseases (owing to the factors discussed in Section 8.2.1), these molecules have served as archetypical scaffolds (generalized structural templates) for the development of many other related AR chemotypes with potentially broad therapeutic application. Over 64 chemically distinct putative AR agonist templates have been reported, including 22 templates with demonstrated in vivo tissue-selectivity for anabolic tissues [i.e. selective AR modulators (SARMs)]. 

As the many research groups active in this field seek new ligand platforms for the optimization of the activity of (Mg) ROP catalysts, several well-defined Mg complexes which do not correspond to the categories previously discussed have been reported in the past 5 years. Although the various ligands considered are obviously not without interest, it must be noted that the complexes built around these scaffolds generally display inferior ability as ROP initiators/catalysts than those introduced in the above sections. 

Step 5 Estimate maintenance costs (after making allowance for tax relieQ over life of structure including access costs such as scaffolding. In general the future maintenance costs must be estimated making allowance for inflation and then discounted to present values see maintenance terms in equation below). 

To perform Diels-Alder reactions on solid phase, the 2(lH)-pyrazinone scaffold is linked to a suitable support via its amide nitrogen atom. While N-l-substituted pyrazinones are readily accessible by the choice of an appropriate amine, it is not possible to prepare N-l-unsubstituted pyrazinones using the general strategy as previously outlined in the introduction. How-... 

The C-6 carboxamide analogues of zanamivir, represented by the general structure 24, provided an avenue to introduce more hydrophobic side-chains onto the dihydropyran scaffold to interact with the hydrophobic regions of subsites S4 and S5 (reviewed in Islam and von Itzstein 2007). The most active tertiary amides (24 = alkyl) showed comparable inhibitory activity to their glycerol side-... 

The concept of minimum AE and maximum Emw is illustrated with the generalized sequence shown in Scheme 4.7 under stoichiometric conditions with complete recovery of reaction solvents, catalysts, and post-reaction materials. Markush structures are used to show both variable R groups and necessarily invariant atoms. This analysis is useful in studying combinatorial hbraries where a constant scaffold structure is selected and then is decorated with, in principle, an unlimited number of possible R groups. 

In the patent literature, Aventis has published a patent application covering hydroxamic acid containing macrocycles (39) with the same general template as the A-formyl-A-hydroxylamine macrocycles described above [114] and GlaxoSmithKline has published an application on macrocyclic PDF inhibitors containing a hydrazide scaffold (40) [115], No data has been published on these inhibitors to date. 

DinickelQI) complexes of general type (781) macrocycles have been studied in detail since the early 1990s.1952-1 (782) is the most prominent scaffold employed, and the structures of its dinickel(II)... 

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