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Background  Sigma (σ) receptors are membrane-bound proteins characterised by an unusual promiscuous ability to bind a wide variety of drugs and their high affinity for typical neuroleptic drugs, such as haloperidol, and their potential as alternative targets for antipsychotic agents. Sigma receptors display diverse biological activities and represent potential fruitful targets for therapeutic development in combating many human diseases. Therefore, they present an interesting avenue for further exploration. It was our goal to evaluate the potential of ring opened spipethiane ( 1 ) analogues as functional ligands (agonists) for σ receptors by chemical modification.    Results  Chemical modification of the core structure of the lead compound, ( 1 ), by replacement of the sulphur atom with a carbonyl group, hydroxyl group and 3-bromobenzylamine with the simultaneous presence of 4-fluorobenzoyl replacing the spirofusion afforded novel potent sigma-1 receptor ligands  7a–f ,  8a–f  and  9d–e . The sigma-1 receptor affinities of  7e ,  8a  and  8f  were slightly lower than that of  1  and their selectivities for this receptor two to threefold greater than that of  1 .    Conclusions  It was found that these compounds have higher selectivities for sigma-1 receptors compared to  1 . Quantitatitive structure–activity relationship studies revealed that sigma-1 binding is driven by hydrophobic interactions.  Graphical abstract   Identified pharmacophore features for sigma binding.Electronic supplementary material  The online version of this article (doi:10.1186/s13065-016-0200-1) contains supplementary material, which is available to authorized users.

chemistry central journal

4-aroylpiperidines and 4-(α-hydroxyphenyl)piperidines as selective sigma-1 receptor ligands: synthesis, preliminary pharmacological evaluation and computational studies