Shroff J R, Elpern B, Kobrin S, Cervoni P
J Med Chem. 1982 Apr;25(4):359-62. doi: 10.1021/jm00346a006.
A series of N-[[(dialkylamino)alkoxyl]phenyl]benzamidines was synthesized and evaluated for hypoglycemic activity in the glucose-primed rat. Structure-activity relationship indicated that N'-phenyl-N-[4-[2(diisopropylamino)-ethoxy]phenyl]benzamidine dihydrobromide (7), N'-(4-chlorophenyl)-N-[4-[2-(diisopropylamino)ethoxy]phenyl]-benzamidine dihydrochloride (31), and N'-phenyl-N-[4-[(diisopropylamino)propoxy]phenyl]benzamidine dihydrobromide (11) are some of the more interesting compounds. A comparison of these hypoglycemic agents with classical standards (tolazamide, phenformin, and buformin) in several experimental models showed that the benzamidines seem to combine in one molecule some of the biological activities of the beta-cytotrophic sulfonylureas and some of the activities of the biguanides.
合成了一系列N-[[(二烷基氨基)烷氧基]苯基]苯甲脒，并在葡萄糖预充的大鼠中评估其降血糖活性。构效关系表明，二氢溴化N'-苯基-N-[4-[2-(二异丙基氨基)乙氧基]苯基]苯甲脒(7)、二盐酸N'-(4-氯苯基)-N-[4-[2-(二异丙基氨基)乙氧基]苯基]苯甲脒(31)和二氢溴化N'-苯基-N-[4-[(二异丙基氨基)丙氧基]苯基]苯甲脒(11)是一些更有趣的化合物。在几个实验模型中，将这些降血糖药物与经典标准药物(甲苯磺丁酰胺、苯乙双胍和丁双胍)进行比较，结果表明，苯甲脒似乎在一个分子中结合了β细胞营养性磺酰脲类药物的一些生物活性和双胍类药物的一些活性。
