Hawes E M, Gorecki D K, Gedir R G
J Med Chem. 1977 Jun;20(6):838-41. doi: 10.1021/jm00216a021.
A variety of 2,3-disubstituted 5,7-dimethyl-1,8-naphthyridines was synthesized and tested in saline-loaded rats for their diuretic properties. The 2-amino-3-carbomethoxy and four 2-amino-3-N-alkylcarbamoyl compounds exhibited significant activity as measured by volume output; however, they were generally less potent than the corresponding 5,7-unsubstituted naphthyridines previously reported. Further screening without saline-loading indicated that the amides lacked kaliuretic properties; while, interestingly, the ester lacked an effect on either urine volume or sodium excretion.
合成了多种2,3-二取代的5,7-二甲基-1,8-萘啶,并在盐水负荷大鼠中测试了它们的利尿特性。通过尿量输出测定,2-氨基-3-甲氧基羰基和四种2-氨基-3-N-烷基氨基甲酰基化合物表现出显著活性;然而,它们的活性通常低于先前报道的相应5,7-未取代萘啶。在无盐水负荷情况下的进一步筛选表明,酰胺类缺乏排钾特性;而有趣的是,酯类对尿量或钠排泄均无影响。