Structure-activity relationships in platelet-activating factor (PAF). 11-From PAF-antagonism to phospholipase A(2) inhibition: syntheses and structure-activity relationships in 1-arylsulfamido-2-alkylpiperazines
| Autor: | Chang-Zhi Dong, Jack Huet, Françoise Heymans, Léon Assogba, Catherine Redeuilh, Carine Mounier, Carine Binisti, Estera Touboul, Jean-Edouard Ombetta, Jean-Jacques Godfroid |
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| Rok vydání: | 2001 |
| Předmět: |
Blood Platelets
Stereochemistry Molecular Conformation Phospholipases A Piperazines chemistry.chemical_compound Inhibitory Concentration 50 Structure-Activity Relationship Phospholipase A2 Amide Catalytic Domain Drug Discovery Moiety Animals Enzyme Inhibitors Platelet Activating Factor Pancreas Sulfamide Chelating Agents Pharmacology Phospholipase A Sulfonamides biology Organic Chemistry Stereoisomerism General Medicine Piperazine chemistry Enzyme inhibitor Lipophilicity biology.protein lipids (amino acids peptides and proteins) Calcium Cattle Rabbits |
| Zdroj: | European journal of medicinal chemistry. 36(10) |
| ISSN: | 0223-5234 |
| Popis: | 1-Benzoyl-2-alkyl piperazines are strong inhibitors of Group I and II secreted PLA2s. An improvement of their activity was obtained by replacing the amide function by a sulfamide and by introduction of electrodonor substituents on the para position of the benzenesulfonyl moiety. Neither the position on one of the carbon of the piperazine ring nor the absolute configuration of this carbon have an effect on the affinity for one or the other group of PLA2, but the lipophilicity remains for these series an essential parameter. In addition structure–activity relationships allow new hypothesis on interaction of these piperazine derivatives with the catalytic site of PLA2s. |
| Databáze: | OpenAIRE |
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