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Literature DB >> 20392639

Discovery of 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-5-(5-fluoropyrimidin-2-yl)benzamide as a potent and CNS penetrable P2X7 receptor antagonist.

Xiangyang Chen¹, Betsy Pierce, Win Naing, Margaret L Grapperhaus, Dennis P Phillion.

Abstract

Focused SAR studies were carried out around 5-heteroaryl and 1-amide portions of the 2-chlorobenzamide scaffold, resulting in the discovery of a potent, metabolically stable and centrally penetrable antagonist against P2X(7) receptor. Copyright 2010 Elsevier Ltd. All rights reserved.

Entities: Chemical Gene

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Year: 2010 PMID： 20392639 DOI： 10.1016/j.bmcl.2010.03.094

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

7 in total

1. P2X receptor antagonists for pain management: examination of binding and physicochemical properties.

Authors: Rebecca J Gum; Brian Wakefield; Michael F Jarvis
Journal: Purinergic Signal Date: 2011-11-16 Impact factor: 3.765

Review 2. Molecular and functional properties of P2X receptors--recent progress and persisting challenges.

Authors: Karina Kaczmarek-Hájek; Eva Lörinczi; Ralf Hausmann; Annette Nicke
Journal: Purinergic Signal Date: 2012-05-01 Impact factor: 3.765

Review 3. Transcriptional control mechanisms associated with the nucleotide receptor P2X7, a critical regulator of immunologic, osteogenic, and neurologic functions.

Authors: Lisa Y Lenertz; Monica L Gavala; Yiming Zhu; Paul J Bertics
Journal: Immunol Res Date: 2011-05 Impact factor: 2.829

7. Preparation of chiral 3-oxocycloalkanecarbonitrile and its derivatives by crystallization-induced diastereomer transformation of ketals with chiral 1,2-diphenylethane-1,2-diol.

Authors: Yohei Yamashita; Daisuke Maki; Shiho Sakurai; Takumi Fuse; Shoji Matsumoto; Motohiro Akazome
Journal: RSC Adv Date: 2018-09-21 Impact factor: 3.361

7 in total

Discovery of 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-5-(5-fluoropyrimidin-2-yl)benzamide as a potent and CNS penetrable P2X7 receptor antagonist.

1. P2X receptor antagonists for pain management: examination of binding and physicochemical properties.

Review 2. Molecular and functional properties of P2X receptors--recent progress and persisting challenges.

Review 3. Transcriptional control mechanisms associated with the nucleotide receptor P2X7, a critical regulator of immunologic, osteogenic, and neurologic functions.

Review 4. Recent Advances in CNS P2X7 Physiology and Pharmacology: Focus on Neuropsychiatric Disorders.

Review 5. The P2X7 Receptor in Inflammatory Diseases: Angel or Demon?

Review 6. Physiological roles and potential therapeutic applications of the P2X7 receptor in inflammation and pain.

7. Preparation of chiral 3-oxocycloalkanecarbonitrile and its derivatives by crystallization-induced diastereomer transformation of ketals with chiral 1,2-diphenylethane-1,2-diol.