AboulWafa O M, el-Metwalli M A
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Egypt.
Arch Pharm (Weinheim). 1992 Sep;325(9):603-8. doi: 10.1002/ardp.19923250915.
Three novel series of benzo[b]thiophene derivatives bearing various hydrazone, hydrazine and 1,3,4-oxadiazole moieties were synthesized as potential antidepressant agents. 22 Compounds were evaluated for their in vitro inhibitory effect on monoamine oxidase enzyme (MAO) type A. Several compounds inhibited MAO stronger than pargyline hydrochloride. Maximum inhibitions of 83% and 90% were observed with 1-benzyl-2-(3-chlorobenzo[b]thienyl-2-carbonyl)hydrazine (24) and 1-[2-(4-chlorophenyl)ethyl]-2-(3-chlorobenzo[b]thienyl-2- carbonyl)hydrazine (35), respectively.
合成了三个带有各种腙、肼和1,3,4-恶二唑部分的新型苯并[b]噻吩衍生物系列，作为潜在的抗抑郁药。评估了22种化合物对A型单胺氧化酶（MAO）的体外抑制作用。几种化合物对MAO的抑制作用比盐酸帕吉林更强。1-苄基-2-(3-氯苯并[b]噻吩-2-羰基)肼（24）和1-[2-(4-氯苯基)乙基]-2-(3-氯苯并[b]噻吩-2-羰基)肼（35）分别观察到最大抑制率为83%和90%。
