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Accepted version

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2017-01-16

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cc-by-nc-nd (c) Elsevier Ltd, 2017
Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/129848

Escape from adamantane: scaffold optimization of novel P2X7 antagonists featuring complex polycycles

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https://doi.org/10.1016/j.bmcl.2017.01.039

Abstract

The adamantane scaffold, despite being widely used in medicinal chemistry, is not devoid of problems. In recent years we have developed new polycyclic scaffolds as surrogates of the adamantane group with encouraging results in multiple targets. As an adamantane scaffold is a common structural feature in several P2X7 receptor antagonists, herein we report the synthesis and pharmacological evaluation of multiple replacement options of adamantane that maintain a good activity profile. Molecular modeling studies support the binding of the compounds to a site close to the central pore, rather than to the ATP-binding site and shed light on the structural requirements for novel P2X7 antagonists.

Subject

Receptors cel·lulars, Medicaments

Subject (English)

Cell receptors, Drugs

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Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)
Articles publicats en revistes (Institut de Biomedicina (IBUB))

Citation

BARNIOL-XICOTA, Marta, et al. Escape from adamantane: scaffold optimization of novel P2X7 antagonists featuring complex polycycles. Bioorganic & Medicinal Chemistry Letters. 2017. Vol. 27, num. 759-763. ISSN 0960-894X. [consulted: 15 of August of 2026]. Available at: https://hdl.handle.net/2445/129848

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