Ergenç N, Capan G, Günay N S, Ozkirimli S, Güngör M, Ozbey S, Kendi E
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Istanbul, Turkey.
Arch Pharm (Weinheim). 1999 Oct;332(10):343-7. doi: 10.1002/(sici)1521-4184(199910)332:10<343::aid-ardp343>3.0.co;2-0.
Conveniently accessible 4-[(2-(3,4-dimethoxyphenyl)ethyl]-3-thiosemicarbazide (2) was converted to new 1-substituted benzylidene/furfurylidene-4- [2-(3,4-dimethoxyphenyl)ethyl]-3-thiosemicarbazides (3) which furnished 2-(substituted benzylidene/furfurylidene) hydrazono-3-[2-(3,4-dimethoxyphenyl)ethyl]thiazolidin-4-ones (4) and 1-(substituted benzylidene/furfurylidene)-amino -3-[2-(3,4-dimethoxyphenyl)ethyl]-2-thioxo-4,5-imidazolidinedio nes (5) on reaction with chloroacetic acid and oxalyl chloride, respectively. The structure of 5 was confirmed by X-ray diffraction studies performed on 5a. 4 and 5 were evaluated for their potentiating effects on pentobarbital induced hypnosis. Most of the compounds caused remarkable increases in pentobarbital sleeping time.
方便可得的4-[(2-(3,4-二甲氧基苯基)乙基]-3-硫代氨基脲(2)被转化为新的1-取代亚苄基/糠叉基-4-[(2-(3,4-二甲氧基苯基)乙基]-3-硫代氨基脲(3),后者分别与氯乙酸和草酰氯反应,生成2-(取代亚苄基/糠叉基)肼基-3-[2-(3,4-二甲氧基苯基)乙基]噻唑烷-4-酮(4)和1-(取代亚苄基/糠叉基)氨基-3-[2-(3,4-二甲氧基苯基)乙基]-2-硫代-4,5-咪唑啉二酮(5)。通过对5a进行X射线衍射研究确定了5的结构。对4和5对戊巴比妥诱导催眠的增强作用进行了评估。大多数化合物使戊巴比妥睡眠时间显著增加。