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在二次大战期间和四十年代的后期,由于氯喹(Ⅰ)等抗疟药的发现以及阿的平(Ⅱ)、氯喹大规模的生产和临床应用,在合成抗疟药的研究方面掀起了寻找新药的热潮,酚类抗疟药即由此而得以发展。主要酚类抗疟药的化学结构通式如下, A=烷基、芳香族氮杂环氨基……—NR_2=脂肪、脂环氨基、氮杂环氨基…… n=0、1。 z(连接位置)=2、3、4位。在这类化合物中,已先后发现氨酚喹(Ⅶ)、咯萘啶(ⅩⅥ)等有效药物。多年来药物化学工作者围绕这类药物做了大量工作,并对其构效关系作了探讨,现整理分述如在二次大战期间和四十年代的后期,由于氯喹(Ⅰ)等抗疟药的发现以及阿的平(Ⅱ)、氯喹大规模的生产和临床应用,在合成抗疟药的研究方面掀起了寻找新药的热潮,酚类抗疟药即由此而得以发展。主要酚类抗疟药的化学结构通式如下, A=烷基、芳香族氮杂环氨基……—NR_2=脂肪、脂环氨基、氮杂环氨基…… n=0、1。 z(连接位置)=2、3、4位。在这类化合物中,已先后发现氨酚喹(Ⅶ)、咯萘啶(ⅩⅥ)等有效药物。多年来药物化学工作者围绕这类药物做了大量工作,并对其构效关系作了探讨,现整理分述如
During the Second World War and the late 1940s, the discovery of chloroquine (Ⅰ) and other antimalarials and the large-scale production and clinical application of aploprid (Ⅱ) and chloroquine set off research on synthetic antimalarial drugs In search of a new drug boom, phenolic antimalarial drugs have been developed. The main phenolic antimalarial chemical formula is as follows, A = alkyl, aromatic heterocyclic nitrogen amino ... ... -NR_2 = fat, alicyclic amino, nitrogen heterocyclic amino ... ... n = 0,1. z (connection position) = 2, 3, and 4 bits. Among these compounds, effective drugs such as paracetamol (Ⅶ) and pyronaridine (ⅩⅥ) have been discovered successively. Over the years, many efforts have been made by drug chemists around these kinds of drugs, and their structure-activity relationship has been explored. For example, during the Second World War and the late 1940s, due to chloroquine (I) and other antimalarial The discovery of drugs, and the large-scale production and clinical application of alprenilol (II) and chloroquine set off a wave of search for new drugs in the research on synthetic antimalarial drugs, thus resulting in the development of phenolic antimalarial drugs. The main phenolic antimalarial chemical formula is as follows, A = alkyl, aromatic heterocyclic nitrogen amino ... ... -NR_2 = fat, alicyclic amino, nitrogen heterocyclic amino ... ... n = 0,1. z (connection position) = 2, 3, and 4 bits. Among these compounds, effective drugs such as paracetamol (Ⅶ) and pyronaridine (ⅩⅥ) have been discovered successively. Over the years, many efforts have been made by drug chemists around these kinds of drugs, and their structure-activity relationship has been explored.