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稠合嘧啶。具有潜在利尿活性的新衍生物的合成。

Fused pyrimidines. Synthesis of new derivatives of potential diuretic activity.

作者信息

Eisa H M, el-Ashmawy M B, Tayel M M, el-Magd S A, el-Kashef H A

机构信息

Department of Medical Chemistry, Faculty of Pharmacy, University of Mansoura, Egypt.

出版信息

Boll Chim Farm. 1996 Nov;135(10):585-90.

PMID:9048447
Abstract

Certain derivatives of quinazoline and its bioisostere pyridopyrimidine carrying important structural features that contribute to diuretic activity, such as sulfonamido, morpholino and chlorophenyl, were prepared as potential diuretic agents. Likewise, some tricyclic 1,2,4-triazolo[3,4-b]quinazolines and pyrido[3,2-d][1,2,4]triazolo[4,3-alpha] pyrimidines with the same features were reported. Nine compounds were tested for the diuretic activity in rats and the results showed that the active compound is 7-chloro-2-methyl-3-phthalimido-4(3H)-quinazoline (4).

摘要

制备了喹唑啉及其生物电子等排体吡啶并嘧啶的某些衍生物作为潜在的利尿剂,这些衍生物带有有助于利尿活性的重要结构特征,如磺酰胺基、吗啉基和氯苯基。同样,也报道了一些具有相同特征的三环1,2,4-三唑并[3,4-b]喹唑啉和吡啶并[3,2-d][1,2,4]三唑并[4,3-α]嘧啶。对九种化合物在大鼠身上进行了利尿活性测试,结果表明活性化合物是7-氯-2-甲基-3-邻苯二甲酰亚胺基-4(3H)-喹唑啉(4)。

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