Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1
Microsomal prostaglandin E(2) synthase (mPGES-1) represents a potential target for novel analgesic and anti-inflammatory agents. High-throughput screening identified several leads of mPGES-1 inhibitors which were further optimized for potency and selectivity. A series of inhibitors bearing a biaryl...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (23), p.6978-6982 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | WU, Tom Y. H JUTEAU, Hélène BRIDEAU, Christine DUCHARME, Yves FRIESEN, Richard W GUIRAL, Sébastien DUFRESNE, Lynn POIRIER, Hugo SALEM, Myriam RIENDEAU, Denis MANCINI, Joseph |
| description | Microsomal prostaglandin E(2) synthase (mPGES-1) represents a potential target for novel analgesic and anti-inflammatory agents. High-throughput screening identified several leads of mPGES-1 inhibitors which were further optimized for potency and selectivity. A series of inhibitors bearing a biaryl imidazole scaffold exhibits excellent inhibition of PGE(2) production in enzymatic and cell-based assays. The synthesis of these molecules and their activities will be discussed. |
| doi_str_mv | 10.1016/j.bmcl.2010.09.129 |
| format | Article |
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The synthesis of these molecules and their activities will be discussed.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2010.09.129</identifier><identifier>PMID: 20965723</identifier><language>eng</language><publisher>Amsterdam: Elsevier</publisher><subject>Animals ; Anti-Inflammatory Agents - chemistry ; Anti-Inflammatory Agents - pharmacology ; Biological and medical sciences ; Bones, joints and connective tissue. Antiinflammatory agents ; Cell Line ; Dinoprostone - antagonists & inhibitors ; Dinoprostone - biosynthesis ; High-Throughput Screening Assays ; Imidazoles - chemistry ; Imidazoles - pharmacology ; Intramolecular Oxidoreductases - antagonists & inhibitors ; Medical sciences ; Mice ; Microsomes - enzymology ; Pharmacology. 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A series of inhibitors bearing a biaryl imidazole scaffold exhibits excellent inhibition of PGE(2) production in enzymatic and cell-based assays. The synthesis of these molecules and their activities will be discussed.</description><subject>Animals</subject><subject>Anti-Inflammatory Agents - chemistry</subject><subject>Anti-Inflammatory Agents - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>Cell Line</subject><subject>Dinoprostone - antagonists & inhibitors</subject><subject>Dinoprostone - biosynthesis</subject><subject>High-Throughput Screening Assays</subject><subject>Imidazoles - chemistry</subject><subject>Imidazoles - pharmacology</subject><subject>Intramolecular Oxidoreductases - antagonists & inhibitors</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Microsomes - enzymology</subject><subject>Pharmacology. 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| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2010-12, Vol.20 (23), p.6978-6982 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Animals Anti-Inflammatory Agents - chemistry Anti-Inflammatory Agents - pharmacology Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Cell Line Dinoprostone - antagonists & inhibitors Dinoprostone - biosynthesis High-Throughput Screening Assays Imidazoles - chemistry Imidazoles - pharmacology Intramolecular Oxidoreductases - antagonists & inhibitors Medical sciences Mice Microsomes - enzymology Pharmacology. Drug treatments Prostaglandin-E Synthases |
| title | Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1 |
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