Parallel synthesis of a series of potentially brain penetrant aminoalkyl benzoimidazoles |
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Authors: | Micco Iolanda Nencini Arianna Quinn Joanna Bothmann Hendrick Ghiron Chiara Padova Alessandro Papini Silvia |
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Affiliation: | Siena Biotech S.p.A., Therapeutic Research, Via Fiorentina 1, Siena 53100, Italy. |
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Abstract: | Alpha7 agonists were identified via GOLD (CCDC) docking in the putative agonist binding site of an alpha7 homology model and a series of aminoalkyl benzoimidazoles was synthesised to obtain potentially brain penetrant drugs. The array was prepared starting from the reaction of ortho-fluoronitrobenzenes with a selection of diamines, followed by reduction of the nitro group to obtain a series of monoalkylated phenylene diamines. N,N'-Carbonyldiimidazole (CDI) mediated acylation, followed by a parallel automated work-up procedure, afforded the monoacylated phenylenediamines which were cyclised under acidic conditions. Parallel work-up and purification afforded the array products in good yields and purities with a robust parallel methodology which will be useful for other libraries. Screening for alpha7 activity revealed compounds with agonist activity for the receptor. |
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