Drug Design 1971
DOI: 10.1016/b978-0-12-060302-2.50008-7
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Modulation of Pharmacokinetics by Molecular Manipulation

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Cited by 37 publications
(7 citation statements)
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“…In small agonist molecules, a differentiation is usually difficult to see between the groups in the molecule primarily involved in the receptor binding, the haptophore, and the groups primarily involved in the receptor activation, the actophore. Groups, especially those involved in pharmacon metabolism and pharmacon transport, are more easily recognizable (Ariens and Simonis, 1974;Ariens, 1971b). In larger bioactive molecules, especially polypeptides, programming for various aspects of the function may be localized in different amino acid sequences, as shown schematically in Fig.…”
Section: Structure and Actionmentioning
confidence: 99%
“…In small agonist molecules, a differentiation is usually difficult to see between the groups in the molecule primarily involved in the receptor binding, the haptophore, and the groups primarily involved in the receptor activation, the actophore. Groups, especially those involved in pharmacon metabolism and pharmacon transport, are more easily recognizable (Ariens and Simonis, 1974;Ariens, 1971b). In larger bioactive molecules, especially polypeptides, programming for various aspects of the function may be localized in different amino acid sequences, as shown schematically in Fig.…”
Section: Structure and Actionmentioning
confidence: 99%
“…79,80 They were, therefore, (unsuccessfully) tested for the treatment of malignant melanoma. 82 Similar efforts were made to fi nd selective cancer chemotherapeutics, and a variety of drugs that are known to accumulate selectively in particular tissues have also been tried. 82 Similar efforts were made to fi nd selective cancer chemotherapeutics, and a variety of drugs that are known to accumulate selectively in particular tissues have also been tried.…”
Section: Site-directed Drug Deliverymentioning
confidence: 99%
“…First, since medicinal chemists are becoming more sensitive to the fact that optimal drug design must take into account Albert, 1973Ariens, 1966Ariens, 1971Palor, 1982Bundgaard, 1982Digenis and Swintosky, 1975Harper, 1959Harper, 1962Higuchi and Stella, 1975Roche, 1977Sinkula and Yalkowsky, 1975Sinkula, 1975Stella, 1973Stella, 1977Stella and Himmelstein, 1980Yalkowsky and Morozowich, 1980 the physical/chemical form of the drug as it pertains to stability, solubility, and other formulation factors, as well as pharmacokinetic factors, such as the transport properties of the drug, it is quite likely that the prodrug approach to optimizing those properties will become an integral part of basic drug design. As such, there is likely to be fewer examples where prodrugs will have to be used in a hindsighted manner to solve problems.…”
Section: Acknowledgementmentioning
confidence: 99%