Nitric oxide donor ß2-agonists:: Furoxan derivatives containing the fenoterol moiety and related furazans
Nitric oxide donor ß2-agonists:: Furoxan derivatives containing the fenoterol moiety and related furazans
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DOI：
10.1021/jm0704595
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发表时间：
2007-10-04
影响因子：
7.3
通讯作者：
Gasco, Alberto
中科院分区：
文献类型：
--
作者：
Buonsanti, M. Federica;Bertinaria, Massimo;Gasco, Alberto
用于治疗的β（2）-肾上腺素能受体激动剂非诺特罗的结构已与氧化呋咱NO-供体部分连接，得到新的NO-供体β（2）-激动剂。为了比较，还合成了不具有释放NO的性质的呋咱类似物。所有化合物在微摩尔或亚微摩尔浓度下对卡巴胆碱预收缩的豚鼠气管环进行测试时，均保持ss（2）激动活性。在氧化呋咱衍生物中，NO对气管舒张的贡献在微摩尔浓度下用产物15 b是明显的。所有新的NO-供体杂交体都能扩张用苯肾上腺素预收缩的大鼠主动脉条。氧化呋咱和呋咱衍生物显示抗氧化活性大于非诺特罗。
The structure of fenoterol, ss(2)-adrenoceptor agonist used in therapy, has been joined with furoxan NO-donor moieties to give new NO-donor ss(2)-agonists. The furazan analogues, devoid of the property to release NO, were also synthesized for comparison. All the compounds retained ss(2)-agonistic activity at micromolar or submicromolar concentration when tested on guinea pig tracheal rings precontracted with carbachol. Among the furoxan derivatives, the NO contribution to trachea relaxation was evident with product 15b at micromolar concentrations. All the new NO-donor hybrids were able to dilate rat aortic strips precontracted with phenylephrine. Both furoxan and furazan derivatives displayed antioxidant activity greater than that of fenoterol.