Conformationally restrained analogs of pravadoline: nanomolar potent, enantioselective,(aminoalkyl) indole agonists of the cannabinoid receptor

TE D'Ambra, KG Estep, MR Bell…

文献索引：D'Ambra; Estep; Bell; Eissenstat; Josef; Ward; Haycock; Baizman; Casiano; Beglin; Chippari; Grego; Kullnig; Daley Journal of Medicinal Chemistry, 1992 , vol. 35, # 1 p. 124 - 135

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被引用次数: 269

摘要

Pravadoline (1) is an (aminoalky1) indole analgesic agent which is an inhibitor of cyclooxygesase and, in contrast to other NSAIDs, inhibits neuronally stimulated contractions in mouse vas deferens (MVD) preparations (ICw= 0.45 pM). A number of conformationally restrained heterocyclic analogues of pravadoline were synthesized in which the morpholinoethyl side chain was tethered to the indole nucleus. Rsstraining the ...