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Synthesis and Benzodiazepine Receptor Affinity of Derivatives of the New Tricyclic Heteroaromatic System Pyrido[3′,2′:5,6]thiopyrano[4,3-c]pyridazin-3(2H,5H)-one

✍ Scribed by Giampaolo Primofiore; Federico Da Settimo; Anna Maria Marini; Francesca Simorini; Concettina La Motta; Sabrina Taliani; Sonia Laneri; Letizia Trincavelli; Claudia Martini

Publisher
John Wiley and Sons
Year
2005
Tongue
English
Weight
125 KB
Volume
338
Category
Article
ISSN
0365-6233

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✦ Synopsis

Abstract

Derivatives 7–13 of a new tricyclic heteroaromatic system, pyrido[3′,2′:5,6]thiopyrano[4,3‐c]pyridazin‐3(2__H__,5__H__)‐one, were prepared as potential ligands at the benzodiazepine receptor, in view of their structural analogy with potent ligands such as the pyrazoloquinolines of the CGS series II, and especially with the benzothiopyrano[4,3‐c]pyridazinones VI. They were obtained starting from the versatile ketones 2,3‐dihydrothiopyrano[2,3‐b]pyridin‐4(4__H__)‐one 1 and the corresponding 7‐methyl derivative 2, via condensation with glyoxylic acid, and reaction of the intermediate acid mixtures with hydrazine or substituted phenylhydrazines. When evaluated for their binding affinity at the benzo diazepine receptor in bovine cortical membranes, the target compounds 8–13 displayed an affinity in the micromolar/submicromolar order. A hypothesis is presented to rationalize these results.

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