Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors

…, F Jovic, M Mesleh, K Phan, J Tamiya, T Vickers…

Index: Chen, Chen; Dyck, Brian; Fleck, Beth A.; Foster, Alan C.; Grey, Jonathan; Jovic, Florence; Mesleh, Michael; Phan, Kasey; Tamiya, Junko; Vickers, Troy; Zhang, Mingzhu Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 4 p. 1346 - 1349

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Citation Number: 15

Abstract

Derivatives of milnacipran were synthesized and studied as monoamine transporter inhibitors. Potent analogs were discovered at NET (9k) and at both NET and SERT (9s and 9u). A pharmacophore model was established based on the conformational analysis of milnacipran in aqueous solution using NMR techniques and was consistent with the SAR results.