Mishra P, Joshi G K, Shakya A K, Agrawal R K, Patnaik G K
Department of Pharmaceutical Sciences, Dr. Harisingh Gour Vishwavidyalaya, Sagar.
Indian J Physiol Pharmacol. 1992 Oct;36(4):247-50.
Nine new 2-(substituted acetyl) amino-5-alkyl-1,3,4-oxadiazoles were synthesised and confirmed on the basis of IR and nitrogen analysis. These were screened for spasmolytic, anti-inflammatory and their effects on blood pressure after determining ALD50. Compounds GK-4 i.e. 2-(diethylaminoacetyl)- amino-5-methyl-1,3,4-oxadiazole and GK-8 i.e. 2-(din-propylamino acetyl)-amino-5-ethyl-1,3,4-oxadiazole were found to be spasmolytic. Compound GK-6 i.e. 2-(diethylaminoacetyl)-amino-5-n-propyl-1,3,4-oxadiazole was found to be a potent hypotensive agent with the effect lasting for more than two hours.
合成了9种新型的2-（取代乙酰基）氨基-5-烷基-1,3,4-恶二唑，并通过红外光谱和氮分析进行了确认。在测定半数致死量后，对这些化合物进行了解痉、抗炎及对血压影响的筛选。发现化合物GK-4即2-（二乙氨基乙酰基）氨基-5-甲基-1,3,4-恶二唑和GK-8即2-（二正丙氨基乙酰基）氨基-5-乙基-1,3,4-恶二唑具有解痉作用。发现化合物GK-6即2-（二乙氨基乙酰基）氨基-5-正丙基-1,3,4-恶二唑是一种有效的降压剂，其作用持续超过两小时。
