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Thiadiazine derivatives R 0660 1,2,4-Benzothiadiazine Derivatives as α 1 and 5-HT 1A Receptor Ligands. -The synthesis and the pharmacological profile of six new benzothiadiazine-arylpiperazines and the effect of some structural modifications on the affinity and selectivity for α1-adrenergic and 5-HT1A serotoninergic receptor subtypes are presented. The best profile of activity at adrenergic system resides in (VIa), which shows high α1D affinity and relevant α 1D selectivity. Compound (IXb) is identified as a novel 5-HT 1A receptor ligand and highly selective over α1D-adrenoceptor subtype. This compound can be considered as a partial agonist at 5-HT1A receptor. -(TAIT*, A.; LUPPI, A.; FRANCHINI, S.; PREZIOSI, E.; PARENTI, C.; BUCCIONI, M.; MARUCCI, G.; LEONARDI, A.; POGGESI, E.; BRASILI, L.; Bioorg. Med. Chem. Lett. 15 (2005) 4, 1185-1188; Dip. Sci. Farm., Univ. Modena, I-41100 Modena, Italy; Eng.) -H. Hoennerscheid 26-103

A series of 2,1,3-and 1,2,4-benzothiadiazine derivatives were synthesized by alkylation via Mitsunobu reaction and evaluated for their antiviral activity against ADV, HHV-6, Cox-B5 and H-CMV. Most of them were active at micromolar level against one or more viral strains. All the molecules studied are poorly cytotoxic (maximum non toxic concentrations were >25µM), except one compound that presents a higher cytotoxicity (maximum non toxic concentration was 6 µM).

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