Synthesis of Benzodioxinopyrroles as selective α2-adrenoceptor antagonists

Kitchin, John R.; Borthwick, Alan D.; Brodie, A. C.; Cherry, P. C.; Crame, Andrew J.; Pipe, Adrian; Procopiou, Panayiotis A.; Seaman, M.A.; Turnbull, Judy

doi:10.1016/0968-0896(95)00143-3

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Benzodioxane Derivatives1

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“…Fluparoxan (115), characterized by a high α 2 /α 1 selectivity ratio of 2630, is a hybrid molecule bearing the benzodioxane and pyrrolidine frames [193].…”

Section: Benzodioxane Derivativesmentioning

confidence: 99%

Agonists and Antagonists Targeting the Different α2-Adrenoceptor Subtypes

Gentili

Pigini²,

Piergentili³

et al. 2007

CTMC

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Chemical and biological strategies have provided evidence for alpha(2)-receptor heterogeneity, to date classified in three different subtypes, alpha(2A), alpha(2B), and alpha(2C). These are widely distributed throughout the body and mediate numerous effects; therefore, the potential therapeutic indications of agonists and antagonists are numerous. Nevertheless, the lack of subtype-selectivity of the well-known compounds represents a major limit for their use. SAR studies may help to design new and more selective drugs.

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“…Fluparoxan (115), characterized by a high α 2 /α 1 selectivity ratio of 2630, is a hybrid molecule bearing the benzodioxane and pyrrolidine frames [193].…”

Section: Benzodioxane Derivativesmentioning

confidence: 99%