Adamantane as a Brain-Directed Drug Carrier for Poorly Absorbed Drug. 2. AZT Derivatives Conjugated with the 1-Adamantane Moiety

Synthesis and evaluation of fluorescent heterocyclic aminoadamantanes as multifunctional neuroprotective agents

“…Amantadine was also shown to increase the blood brain barrier (BBB) permeability of privileged moieties conjugated to it, which is desirable for greater CNS drug effect. 29 Furthermore in a previous study done in our laboratories, 28 fluorescent ligands structurally related to 7-nitroindazole (7-NI; a potent selective nNOS inhibitor), 30,31 were conjugated to amantadine and were found to have moderate to potent NOS inhibitory activity. Fluorescent ligands structurally similar to 7-NI were developed using different bioisosteric substitutions while maintaining certain pharmacophoric groups.…”

Ester Derivatives of Nucleoside Inhibitors of Reverse Transcriptase: 1. Molecular Transport Systems for 3′-Azido-3′-Deoxythymidine and 2′,3′-Didehydro-3′-Deoxythymidine

“…Brain is protected from water-soluble substances by BBB, which blocks the penetration of polar molecules to the brain tissues, including the antiviral nucleosides. Various chemical methods were suggested to enhance the delivery of nucleosides to the brain tissues [47][48][49]. One of the best developed systems of the Scheme 8.…”

Polycyclic Compounds: Ideal Drug Scaffolds for the Design of Multiple Mechanism Drugs?

“…This conjugate significantly improved blood-brain barrier penetration of the drug into the CNS. 75 The adamantyl structure has yielded many compounds in the past 50 years directed toward many different drug targets. FIG.…”