synthesis and chemiluminescent high throughput screening for inhibition of acetylcholinesterase...

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2006 Thiazole derivatives R 0260 Synthesis and Chemiluminescent High Throughput Screening for Inhibition of Acetylcholinesterase Activity by Imidazo[2,1-b]thiazole Derivatives. — A new se- ries of imidazothiazole derivatives with different spacers (8 examples) is synthesized and evaluated as acetylcholinesterase inhibitors. Compounds (III) show no appreciable inhibitory potency probably due to their low solubility in water while the corresponding quaternized derivatives (V) are good inhibitors with activities related to the spacer em- ployed. — (ANDREANI*, A.; GRANAIOLA, M.; GUARDIGLI, M.; LEONI, A.; LOCATELLI, A.; MORIGI, R.; RAMBALDI, M.; RODA, A.; Eur. J. Med. Chem. 40 (2005) 12, 1331-1334; Dip. Sci. Farm., Univ. Bologna, I-40126 Bologna, Italy; Eng.) — M. Schroeter 17- 129

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2006

Thiazole derivativesR 0260 Synthesis and Chemiluminescent High Throughput Screening for Inhibition of

Acetylcholinesterase Activity by Imidazo[2,1-b]thiazole Derivatives. — A new se-ries of imidazothiazole derivatives with different spacers (8 examples) is synthesized and evaluated as acetylcholinesterase inhibitors. Compounds (III) show no appreciable inhibitory potency probably due to their low solubility in water while the corresponding quaternized derivatives (V) are good inhibitors with activities related to the spacer em-ployed. — (ANDREANI*, A.; GRANAIOLA, M.; GUARDIGLI, M.; LEONI, A.; LOCATELLI, A.; MORIGI, R.; RAMBALDI, M.; RODA, A.; Eur. J. Med. Chem. 40 (2005) 12, 1331-1334; Dip. Sci. Farm., Univ. Bologna, I-40126 Bologna, Italy; Eng.) — M. Schroeter

17- 129