Pyrrolidine inhibitors of human cytosolic phospholipase A2. Part 2
| Autor: | Yasushi Murakami, Katsutoshi Yamada, Shozo Nakamoto, Takayuki Okuno, Takashi Ono, Koichi Nishi, Kaoru Seno |
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| Rok vydání: | 2001 |
| Předmět: |
chemistry.chemical_classification
Phospholipase A biology Thromboxane Stereochemistry medicine.medical_treatment Organic Chemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Pyrrolidine chemistry.chemical_compound Cytosol Enzyme Phospholipase A2 chemistry Drug Discovery medicine biology.protein Molecular Medicine Arachidonic acid Molecular Biology Prostaglandin E |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 11:587-590 |
| ISSN: | 0960-894X |
| Popis: | We synthesized a potent and crystallized human cytosolic phospholipase A 2 α inhibitor, pyrrophenone ( 6 ) which inhibits the isolated enzyme with an IC 50 value of 4.2 nM. Pyrrophenone shows potent inhibition of arachidonic acid release, prostaglandin E 2 , thromboxane B 2 , and leukotriene B 4 formation in human whole blood. The magnitudes of prostaglandin E 2 and thromboxane B 2 inhibition are the same as those of indomethacin. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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