Preparation of two Cyclobutadiene-steroid derivatives Theoretical Analysis of its Interaction with the μ, d, and k Opiod-receptors
| Autor: | Figueroa-Valverde Lauro, Rosas-Nexticapa Marcela, Mateu-Armand Virginia, Diaz-Cedillo Francisco, Hau-Heredia Lenin, Lopez-Ramos Maria, Garcia-Cervera Elodia, Pool-Gomez Eduardo, Cauich-Carrillo Regina |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
chemistry.chemical_classification Stereochemistry medicine.medical_treatment Supramolecular chemistry Ornamental horticulture General Chemistry Radiation chemistry 010402 general chemistry 01 natural sciences Biochemistry 0104 chemical sciences Steroid Coordination complex 03 medical and health sciences chemistry.chemical_compound 030104 developmental biology chemistry Drug Discovery Theoretical chemistry medicine Environmental Chemistry Cyclobutadiene Receptor |
| Zdroj: | Oriental Journal of Chemistry. 34:2689-2702 |
| ISSN: | 2231-5039 0970-020X |
| DOI: | 10.13005/ojc/340601 |
| Popis: | The objective of this investigation was to develop two cyclobutadiene-steroid derivatives (compounds 6 or 7) to evaluate its theoretical interaction on µ, d, and k opioid-receptors. The synthesis of 6 or 7 was carried out using a series of reactions which involves. 1) addition/cyclization: 2) imination, 3) etherification and 4) oxy-functionalization. Chemical structure of all compounds was confirmed using elemental analysis and NMR spectra. In addition, a theoretical analysis on the interaction of compounds 6 or 7 with µ, d, and k opioid-receptors was evaluated using a docking model. The results showed that 6 or 7 may interact with different type of amino acids residues on surface of the µ, d, and k opioid-receptors. Other data, indicated that inhibition constant (Ki) involved in the interaction of compounds 6 or 7 with k receptor was less compared with the Ki present in the interaction with µ, d, receptors. These data indicated that 1) compounds 6 or 7 show a high affinity by k-receptor; 2) the cyclobutadiene analogs are particularly interesting, because these drugs may constitute a novel therapy for pain. |
| Databáze: | OpenAIRE |
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