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为了寻找比消炎痛(1)疗效好、毒性低和易于忍受的抗炎药物,作者从Hansch报道的芳香化合物取代基常数表中推算出化合物(1)结构中以叠氮基替代N-苯甲酰基中的4位氯原子最为合适。这种改变已在苯并二氮杂(艹卓)类药物研究中取得成效。本文即报道zido-metacin(2)的合成及其初步药理结果。
In an effort to find anti-inflammatory drugs that are more potent, less toxic and tolerable than indomethacin (1), the authors deduced from the list of substituent constants of aromatic compounds reported by Hansch that the azide-substituted N-benzyl The 4-position chlorine atom in the acyl group is most suitable. This change has been in the benzodiazepine drug research results. This article reports the synthesis of zido-metacin (2) and its preliminary pharmacological results.