The potential of P2X7 receptors as a therapeutic target, including inflammation and tumour progression

G Burnstock, GE Knight - Purinergic signalling, 2018 - Springer
Seven P2X ion channel nucleotide receptor subtypes have been cloned and characterised.
P2X7 receptors (P2X7R) are unusual in that there are extra amino acids in the intracellular …

Applications of fluorine to the construction of bioisosteric elements for the purposes of novel drug discovery

P Richardson - Expert Opinion on Drug Discovery, 2021 - Taylor & Francis
Introduction There continues to be an exponential rise in the number of small molecule
drugs that contain either a fluorine atom or a fluorinated fragment. While the unique …

Challenges and opportunities in central nervous system drug discovery

JJ Danon, TA Reekie, M Kassiou - Trends in Chemistry, 2019 - cell.com
The development of new drugs for disorders of the central nervous system (CNS) presents
unique challenges when compared with other disease areas. These include an incomplete …

From lead to clinic: A review of the structural design of P2X7R antagonists

R Zhang, N Li, M Zhao, M Tang, X Jiang, X Cai… - European Journal of …, 2023 - Elsevier
Abstract P2X7R, which is a member of the purinergic P2 receptor family, is widely expressed
in many immune cells, such as macrophages, lymphocytes, monocytes, and neutrophils …

Pharmacological Evaluation of Novel Bioisosteres of an Adamantanyl Benzamide P2X7 Receptor Antagonist

SM Wilkinson, ML Barron… - ACS chemical …, 2017 - ACS Publications
Adamantanyl benzamide 1 was identified as a potent P2X7R antagonist but failed to
progress further due to poor metabolic stability. We describe the synthesis and SAR of a …

1-Aryl-1H-and 2-aryl-2H-1, 2, 3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo

DTG Gonzaga, LBG Ferreira, TEMM Costa… - European Journal of …, 2017 - Elsevier
Abstract Fifty-one 1, 2, 3-triazole derivatives were synthesized and evaluated with respect to
P2X7 receptor (P2X7R) activity and its associated pore. These triazoles were screened in …

ATP-activated P2X7 receptor in the pathophysiology of mood disorders and as an emerging target for the development of novel antidepressant therapeutics

L Wei, SAS Mortadza, J Yan, L Zhang, L Wang… - Neuroscience & …, 2018 - Elsevier
Mood disorders are a group of psychiatric conditions that represent leading global disease
burdens. Increasing evidence from clinical and preclinical studies supports that innate …

Theoretical studies on cycloaddition reactions of N-allyl substituted polycyclic Isoindole-1, 3-dione with nitrones and nitrile oxides

B Donkor, E Opoku, A Aniagyei - Computational and Theoretical Chemistry, 2022 - Elsevier
Bridged polycyclic molecular skeletons and related systems are key structural motifs in
medicinal chemistry. The most efficient and widely accepted method for the syntheses of the …

P2X7 receptor antagonists for the treatment of systemic inflammatory disorders

CF Gelin, A Bhattacharya, MA Letavic - Progress in Medicinal Chemistry, 2020 - Elsevier
P2X7 has continued to be a target of immense interest since it is implicated in several
peripheral and central nervous system disorders that result from inflammation. This review …

1, 3-Dipolar cycloaddition of N-allyl substituted polycyclic derivatives of isoindole-1, 3-dione with nitrones and nitrile oxides: An experimental and theoretical …

MM Efremova, AP Molchanov, AS Novikov, GL Starova… - Tetrahedron, 2020 - Elsevier
Cycloaddition reactions of N-allyl substituted polycyclic derivatives of isoindole-1, 3-dione
with nitrones proceeds regio-and stereoselectively on the double bond of the N-allyl …