Synthesis and structure_activity relationship studies of theophylline analogs

• Authors: ANANTHALAKSHMI Kethireddy V. V.; BARTL Tomáš; AZIZA Mohammed H.; NOVOTNÝ Ladislav; MAREK Radek; BENEŠ Luděk; KOMBIAN Samuel B.
• Year of publication: 2008
• Type: Article in Periodical
• Magazine / Source: Bioorganic & Medicinal Chemistry
• MU Faculty or unit: Faculty of Science
• Field: Biochemistry
• Keywords: Hippocampus; Acetylcholine receptors; Dementia; Nootropic; Theophylline analogs
• Description: We synthesized several theophylline analogs and tested the hypothesis that these compounds may be nootropic or cognitive enhancers by examining their effects on evoked population spikes recorded extracellularly in the CA1 region of the rat hippocampus. Whereas the length of the carbon chain on N7 had no effect, different size of the terminal lactam ring strongly influenced neuroactivity. Our results suggest that hexahydroazepin-2-one analogs have potential for further development as cognitive enhancers.

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