Synthesis and pharmacological evaluation of pentacyclic 6a,7-dihydrodiindole and 2,3-dihydrodiindole derivatives as novel melatoninergic ligands |
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Authors: | Attia Mohamed I Witt-Enderby Paula A Julius Justin |
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Affiliation: | Pharmaceutical Institute, Pharmaceutical Chemistry Division, University of Würzburg, Am Hubland, 97074 Würzburg, Germany. atia@pzlc.uni-wuerzburg.de |
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Abstract: | The synthesis of novel melatonin analogues 3a and 4a-c designed as melatonin receptor ligands is described. Among the newly synthesized ligands, 2-((S)-2-hydroxymethylindolin-1-ylmethyl)-melatonin 4b displayed the highest affinity for MT(1) receptors (K(i)=9.8 nM) and for MT(2) subtype (K(i)=7.8 nM), whereas the rigid pentacyclic ligand 3 showed the highest selectivity towards the MT(2) receptor subtype (K(i)=319.3 nM for MT(1) and K(i)=65.2 nM for MT(2)). |
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