Facile synthetic approach towards vasorelaxant active 4-hydroxyquinazoline-4-carboxamides

Marian N. Aziz; Siva S. Panda; ElSayed M. Shalaby; Nehmedo G. Fawzy; Adel S. Girgis

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Facile synthetic approach towards vasorelaxant active 4-hydroxyquinazoline-4-carboxamides

机译：简便的合成方法治疗血管舒张活性的4-羟基喹唑啉-4-羧酰胺

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A Facile synthetic approach is reported towards 4-hydroxyquinazoline-4-carboxamides 13a–i through ring expansion of 2,3-dioxoindoline-1-carboxamides 10a–c during secondary amine 11a–d nucleophilic reaction. Single crystal X-ray studies of 10c and 13d support the structures. Some of the synthesized quinazolinecarboxamides 13 show promising vasorelaxant properties with potency higher than that of Doxazosin through the pre-contracted (norepinephrine hydrochloride) rat aorta standard bioassay. Good molecular models (2D-QSAR, pharmacophore) describe the biological observations.

机译：据报道，在仲胺11a-d亲核反应过程中，通过2,3-二氧代吲哚啉-1-羧酰胺10a-c的扩环，可以轻松合成4-羟基喹唑啉-4-羧酰胺13a-i。 10c和13d的单晶X射线研究证明了这种结构。通过预收缩（去甲肾上腺素盐酸盐）大鼠主动脉标准生物测定法，一些合成的喹唑啉羧酰胺13显示出有希望的血管舒张性质，其效力高于多沙唑嗪。好的分子模型（2D-QSAR，药效团）描述了生物学观察。

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《RSC Advances》 |2019年第49期|共7页
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Marian N. Aziz; Siva S. Panda; ElSayed M. Shalaby; Nehmedo G. Fawzy; Adel S. Girgis;
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1. Facile synthetic approach towards vasorelaxant active 4-hydroxyquinazoline-4-carboxamides [J] . RSC Advances . 2019,第49期

机译：朝向血管内活性4-羟基喹唑啉-4-甲酰胺的容易合成方法
2. Facile synthetic approach towards vasorelaxant active 4-hydroxyquinazoline-4-carboxamides [J] . Marian N. Aziz, Siva S. Panda, ElSayed M. Shalaby, RSC Advances . 2019,第49期

机译：简便的合成方法治疗血管舒张活性的4-羟基喹唑啉-4-羧酰胺
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Facile synthetic approach towards vasorelaxant active 4-hydroxyquinazoline-4-carboxamides

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