
Journal of Medicinal Chemistry p. 979 - 981 (1985)
Update date:2022-08-30
Topics:
Bundgaard
Falch
Larsen
Mosher
Mikkelson
Pilocarpic acid esters are shown to be potentially useful prodrugs of pilocarpine with the aim of improving its ocular delivery characteristics. The diesters are of particular interest since they combine an enhanced bioavailability and greatly prolonged duration of activity with a high stability in eye-drop formulation. The proprodrug or sequential cascade concept utilized in the design of these derivatives, involving and enzymatic cleavage mechanisms prior to the occurrence of a chemical (nonenzymatic) reaction, may also be of more general interest in prodrug design.
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Doi:10.1021/jp993894m
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