A divergent SAR study allows optimization of a potent 5-HT2c inhibitor to a promising antimalarial scaffold

…, JC de la Rosa, MB Jiménez-Díaz, T Mulet…

Index: Calderon, Felix; Vidal-Mas, Jaume; Burrows, Jeremy; De La Rosa, Juan Carlos; Jimenez-Diaz, Maria Belen; Mulet, Teresa; Prats, Sara; Solana, Jorge; Witty, Michael; Gamo, Francisco Javier; Fernandez, Esther ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 5 p. 373 - 377

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Citation Number: 12

Abstract

From the 13 533 chemical structures published by GlaxoSmithKline in 2010, we identified 47 quality starting points for lead optimization. One of the most promising hits was the TCMDC- 139046, a molecule presenting an indoline core, which is well-known for its anxiolytic properties by interacting with serotonin antagonist receptors 5-HT2. The inhibition of this target will complicate the clinical development of these compounds as antimalarials. ...

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