Modification Strategies

PK Banerjee, GL Amidon. Physicochemical property modification strategies based on enzyme substrate specificities I Rationale, synthesis, and pharmaceutical properties of aspirin derivatives. J Pharm Sci 70 1299, 1981. 

PK Banerjee, GL Amidon. Physicochemical property modification strategies based... 

In practice, surface modifications are restricted to sensors of the ATR- or FEWS-type. For other transducer layouts, the sample - radiation interaction is less localised, making a modification difficult to impossible. Depending on the analytes and the environment of the sensor, two basic surface modification strategies can be used to enhance the function of vibrational spectroscopic optical chemical sensors. The functional layers can either be... 

This same type of modification strategy also can be used to create highly reactive groups from functionalities of rather low reactivity. For instance, carbohydrate chains on glycoproteins can be modified with sodium periodate to transform their rather unreactive hydroxyl groups into highly reactive aldehydes. Similarly, cystine or disulfide residues in proteins can be selectively reduced to form active sulfhydryls, or 5 -phosphate groups of DNA can be transformed to yield modifiable amines. 

Abstract In this chapter, recent progress in the synthesis, crystal structures and physical properties of monomeric phthalocyanines (Pcs) is summarized and analysed. The strategies for synthesis and modification of Pcs include axial coordination of central metal ions, peripheral substitution of Pc rings and the ionization of Pcs. The crystal structures of various typical Pcs, especially the effects of different synthetic and modification strategies on the supramolecular assemblies of Pcs via %—% interactions between Pc rings, are discussed in detail. Finally, the UV-vis spectroscopic, conducting, magnetic and catalytic properties of some Pcs with crystal structures are presented briefly, and the correlations between various properties and the molecular structure discussed. 

Generally, the above three methods are effective synthetic and modification strategies for preparing soluble Pcs and tuning their properties. In the actual process of synthesizing soluble Pcs, the most effective strategy is certainly the combination of all the three methods and many Pcs have actually been synthesized based on this consideration [73-77]. 

Therefore, surface modification strategies for the formation of direct silicon-carbon bonds require, first, a special pre-treatment of the silicon surface to prevent oxidation and, second, an activation of the silicon surface for subsequent reaction with organic moieties. This has been achieved by treatment of the silicon surface with hydrofluoric acid to generate a hydrogen-terminated Si(lll) surface, which can further react with unsaturated co-functionahzed alkenes in the presence of UV irradiation or by thermal activation [27,44,45]. Using this method, carboxylic acid modified silicon substrates have been successfully generated and coupled to thiol modified ONDs via a polylysine/sulfosuccinimidyl 4-(M-maleimidomethyl)-cyclohexane-l-carboxylate couphng (Fig. 12). 

The success of PEG-ADA led to other applications of this surface-modification strategy. In particular, the ability of PEG to increase the hydrodynamic size of IL-2... 

As stated previously, peptidomimetic drug discovery was first advanced by molecular design concepts and chemical modification strategies focused on... 

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