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本文用三种不同的方法分别合成了五个尚未见文献报道的1,2-二氢-2-氧代喹啉-4-羧酸酯,同时改进文献方法合成了DL-α-氨基-β-[4-(1,2-二氢-2-氧代喹啉)]丙酸及其中间体。用106只小鼠测定了以上化合物的生理活性,腹腔注射(25～50mg/kg)均未见小鼠行为异常,全部动物均未见注射后24h内死亡现象,其中若干衍生物(25mg/kg,i.p.)可使小鼠呈现适度的降低肛温和呼吸频率生理效应,化合物Ⅴ与Ⅵ作用最显著。Ⅵ与戊巴比妥呈现协同作用表明该类化合物有可能具有外源性促眠效应。
In this paper, five unreported 1,2-dihydro-2-oxoquinoline-4-carboxylates have been synthesized by three different methods. At the same time, literature methods were used to synthesize DL-α-amino- - [4- (1,2-dihydro-2-oxoquinoline)] propionic acid and intermediates thereof. The physiological activities of the above compounds were determined in 106 mice. There was no behavioral abnormalities in mice by intraperitoneal injection (25-50 mg / kg), and no animals died within 24 hours after injection. Some of the derivatives (25 mg / kg , ip) can reduce the rectal temperature and respiratory rate of mice showed a moderate physiological effects, the most significant role of compounds Ⅴ and Ⅵ. Ⅵ and pentobarbital synergies show that these compounds may have exogenous hypnotic effect.