Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 1: Initial structure-activity relationship studies of a hit from a high throughput screening
| Autor: | Hiroyuki Kai, Natsuki Ishizuka, Masaharu Kume, Fumiyo Takahashi, Takayuki Kameyama, Shunji Shinohara, Maki Tomari, Shinji Shimada, Naotake Kobayashi, Yoshikazu Tanaka, Haruki Kinoshita, Miho Oohara, Hiroyuki Tobinaga, Masahide Ohdan |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Purinergic P2X Receptor Antagonists Clinical Biochemistry Analgesic Pharmaceutical Science Moderate activity Pharmacology Biochemistry Structure-Activity Relationship 03 medical and health sciences Cell Line Tumor Drug Discovery medicine Animals Structure–activity relationship Pyrroles Receptor Molecular Biology Ion channel Analgesics Molecular Structure Chemistry Organic Chemistry Purinergic receptor Chronic pain medicine.disease High-Throughput Screening Assays Rats body regions 030104 developmental biology Molecular Medicine P2X3 Receptor |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 28:2338-2342 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2017.04.060 |
| Popis: | The P2X3 receptor is primarily expressed in the peripheral sensory nerves, and therefore, antagonists of this receptor may be useful for the treatment of chronic pain. Pyrrolinone derivatives have been identified as a novel class of P2X3 receptor antagonists. A lead structure with moderate activity was discovered through a high-throughput screening assay. A structure-activity study led to the discovery of several P2X3 receptor antagonists. Compound 34 showed potent and specific antagonistic activity and analgesic efficacy. |
| Databáze: | OpenAIRE |
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