平喘药物研究  Ⅱ.一些ω-(3-羟基-1,4-萘醌基-2)-烷基羧酸及2-羟基-1,4-萘醌Mannich碱的合成

STUDIES ON ANTIASTHMATIC AGENTS II. SYNTHESIS OF SOME ω-(3-HYDROXY-1, 4-NAPHTHO- QUINONYL-2)-ALKANOIC ACIDS AND MANNICH BASES OF 2-HYDROXY-l, 4-NAPHTHOQUINONE

摘要: 前曾合成一系列4-氧-4-氢-1-苯骈吡喃-3-甲醛化合物,证明有明显的平喘作用。在前文研究基础上,我们继续报告若干ω-(3-羟基-1,4-萘醌基-2)-烷基羧酸及2-羟基-1,4-萘醌Mannich碱的合成。这些化合物结构上既保存了前文报告的有效化合物II的特点,又类似于一些中草药平喘有效成分,而且尚能制成水溶性盐应用。药理试验正在进行中。

Abstract: To develop novel antiasthmatic agents other than the catecholamine group and without effect on adrenergic β₂ receptor, a series of naphthoquinone compounds (Ⅳ and Ⅴ) were synthesized. These compounds are structurally related both to a potent chromone compound (Ⅱ) reported in our previous paper and to some antiasthmatic active principles of Chinese traditional herbs. In addition, they can also be prepared as water-soluble salts for clinical use. The antiasthmatic tests of compounds Ⅳ and Ⅴ are in progress.