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2-官能化1,4-苯二氮䓬衍生物作为潜在的类似美他西泮抗焦虑剂的合成及受体结合研究

Synthesis and receptor binding studies of 2-functionalized 1,4-benzodiazepine derivatives as potential metaclazepam-like antianxiety agents.

作者信息

Anzini M, Cappelli A, Vomero S, Cagnotto A, Skorupska M

机构信息

Dipartimento Farmaco Chimico Tecnologico, Università Degli Studi di Siena, Italy.

出版信息

Farmaco. 1993 Jul;48(7):897-905.

PMID:8104405
Abstract

The synthesis of 7-chloro-2,3-dihydro-2-(2-methoxyethyl)-1-methyl-5-phenyl- 1H-1,4-benzodiazepine (2) is described. While the metaclazepam-like compound 2 showed an affinity for benzodiazepine receptor central type (CBZRs) comparable to that of metaclazepam (1a), its intermediates bearing the exocyclic double bond resulted more active.

摘要

描述了7-氯-2,3-二氢-2-(2-甲氧基乙基)-1-甲基-5-苯基-1H-1,4-苯并二氮杂䓬(2)的合成。虽然类美他西泮化合物2对中枢型苯二氮䓬受体(CBZRs)的亲和力与美他西泮(1a)相当，但其带有环外双键的中间体活性更高。

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