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Imidazo-thiazine, -diazinone and -diazepinone derivatives. Synthesis, structure and benzodiazepine receptor binding.

Abstract：

:In our search for new compounds acting on benzodiazepine receptors among the fused 2-thiohydantoin derivatives, a series of arylidene imidazo[2,1-b]thiazines was synthesized. The 1,2- and 2,3- cyclized derivatives of mono- and di-substituted Z-5-arylidene-2-thiohydantoins were examined (the X-ray crystal structure of Z-2-cinnamylidene-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazin-3(2H)-one was determined) and compared with the diphenyl derivatives. To investigate the influence of the type of annelated ring on the biological activity, imidazo[2,1-b]pyrimidinone and imidazo[2,1-b]diazepinone derivatives were obtained. The method used in annelation (1,2- and 2,3-cyclized isomers with the exception of fused arylidene imidazothiazines), the substitution pattern (arylidene towards diphenyl) as well as the character of the annelated ring had minor influence on the benzodiazepine receptor affinity of the investigated compounds. It appears that the greatest influence on the biological activity has the character and position of the substituents on the arylidene ring.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Kieć-Kononowicz K,Karolak-Wojciechowska J,Müller CE,Schumacher B,Pekala E,Szymańska E

doi

10.1016/s0223-5234(01)01239-9

subject

Has Abstract

pub_date

2001-05-01 00:00:00

pages

407-19

issue

5

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(01)01239-9

journal_volume

36

pub_type

杂志文章

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