Synthesis of 6a,7b-dihydroxyvouacapan-17b-oic acid derivatives. Part IV: mannich base derivatives and its activities on the electrically stimulated Guinea-pig ileum preparation

Synthesis of 6a,7b-dihydroxyvouacapan-17b-oic acid derivatives. Part IV: mannich base derivatives and its activities on the electrically stimulated Guinea-pig ileum preparation
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DOI:
10.1590/s0103-50532002000600016
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发表时间:
2002-11-01
影响因子:
1.4
通讯作者:
Piló-Veloso, Dorila
Piló-Veloso, Dorila
中科院分区:
化学4区
文献类型:
--
作者:
Belinelo, Valdenir J.;Reis, Genuína T.;Piló-Veloso, Dorila

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从Pterodon polygalaeflorus Benth果实中分离的呋喃二萜6 α,7 β-二羟基vouacapan-17 β-酸(ADV,1)在当前啮齿动物实验模型中呈现镇痛活性。为了收集生物学研究的数据,获得了六种新的酰胺衍生物,其在呋喃环中被烷基胺基团取代,通过与预先形成的亚胺盐的Mannich反应制备。这些衍生物进行了初步的体外药理学试验评价。其结构经IR、H-1和C-13 NMR确证。
The furanditerpene 6alpha,7beta-dihydroxyvouacapan-17beta-oic acid (ADV, 1), isolated from Pterodon polygalaeflorus Benth fruits, presents analgesic activity in current rodent experimental models. With the aim to gather data for biological studies it were obtained six new amide derivatives substituted in the furan ring with alkylamine groups, prepared by the Mannich reaction with preformed iminium salts. These derivatives were evaluated in a preliminary in vitro pharmacological test. Structures were determined by spectroscopic data of IR, H-1 and C-13 NMR.