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Delivery tissue-selective

Tissue-selective activation of classical prodrugs Site-specific delivery of ad hoc chemical systems... [Pg.24]

Turning our attention first to alkyl carbamates of cyclic amides, we find interesting attempts to improve the pharmaceutical and pharmacokinetic properties of 5-fluorouracil (8.152, R = H) [194-196], This antitumor agent, while clinically useful, suffers from poor water solubility, unsatisfactory delivery properties and low tissue selectivity. A variety of prodrug candidates were prepared, in particular the alkyl and aryl carbamates presented in Table 8.12. With the exception of the more-lipophilic derivatives, these compounds exhibited somewhat improved water solubility. More importantly, both rectal and oral bioavailability were markedly improved. The activation... [Pg.513]


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See also in sourсe #XX -- [ Pg.568 ]




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Selective tissue selectivity

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