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- Title
Preparation of two Cyclobutadiene-steroid derivatives Theoretical Analysis of its Interaction with the μ, δ, and k Opioid-receptors.
- Authors
LAURO, FIGUEROA-VALVERDE; MARCELA, ROSAS-NEXTICAPA; VIRGINIA, MATEU-ARMAND; FRANCISCO, DIAZ-CEDILLO; LENIN, HAU-HEREDIA; MARIA, LOPEZ-RAMOS; ELODIA, GARCIA-CERVERA; EDUARDO, POOL-GOMEZ; REGINA, CAUICH-CARRILLO
- Abstract
The objective of this investigation was to develop two cyclobutadiene-steroid derivatives (compounds 6 or 7) to evaluate its theoretical interaction on μ, δ 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, δ 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, δ 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, δ 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.
- Subjects
CYCLOBUTADIENE; STEROIDS; OPIOID receptors; AMINO acids; ETHERIFICATION; CHEMICAL structure
- Publication
Oriental Journal of Chemistry, 2018, Vol 34, Issue 6, p2689
- ISSN
0970-020X
- Publication type
Article
- DOI
10.13005/ojc/340601