Can silicon make an excellent drug even better? An in vitro and in vivo head-to-head comparison between loperamide and its silicon analogue sila-loperamide.

Abstract

Loperamide (1a), an opioid receptor agonist, is in clinical use as an antidiarrheal agent. Carbon/silicon exchange (sila-substitution) at the 4-position of the piperidine ring of 1a (R3 COH→R3 SiOH) leads to sila-loperamide (1b). Sila-loperamide was synthesized in a multistep procedure, starting from triethoxyvinylsilane and taking advantage of the 4… (More)
DOI: 10.1002/cmdc.201500040

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Cite this paper

@article{Geyer2015CanSM, title={Can silicon make an excellent drug even better? An in vitro and in vivo head-to-head comparison between loperamide and its silicon analogue sila-loperamide.}, author={Marcel Geyer and Eric Wellner and Ulrik Jurva and Sebastian Saloman and Duncan Armstrong and Reinhold Tacke}, journal={ChemMedChem}, year={2015}, volume={10 5}, pages={911-24} }