Sorba G, Fruttero R, Di Stilo A, Gasco A, Orsetti M
Dipartimento die Scienza e Tecnologia del Farmaco-Università di Torino, Italy.
Arch Pharm (Weinheim). 1992 Mar;325(3):151-5. doi: 10.1002/ardp.19923250304.
Analogues of 3-amino-4-[2-[(5-dimethylaminomethyl-2-furyl)methylthio]ethylamino] furazan (1) containing carbonyl groups joined to the amino functions linked to the furazan system have been synthetized and investigated for their H2-antagonist properties on the isolated guinea pig right atrium. The presence of the carbonyl group lowers the activity in respect to the corresponding leads. The decrease in activity is only by 1-2 orders of magnitude in the 3-acylamino-furazan series versus inactivity in the 4-acylamino isomers and in the diacylated series.
已合成了3-氨基-4-[2-[(5-二甲基氨基甲基-2-呋喃基)甲硫基]乙氨基]呋咱(1)的类似物，这些类似物含有与连接到呋咱系统的氨基官能团相连的羰基，并在离体豚鼠右心房上研究了它们的H2拮抗剂特性。羰基的存在相对于相应的先导化合物降低了活性。在3-酰基氨基-呋咱系列中，活性仅降低1-2个数量级，而在4-酰基氨基异构体和二酰化系列中则无活性。
