Synthesis of piperidine derivatives with a quinazoline ring system as potential antihypertensive agents.
作者:HARUKI TAKAI、HIROYUKI OBASE、MASAYUKI TERANISHI、AKIRA KARASAWA、KAZUHIRO KUBO、KATSUICHI SHUTO、YUTAKA KASUYA、KOKI SHIGENOBU
DOI:10.1248/cpb.34.1907
日期:——
A series of piperidine derivatives with a 2-oxo-1, 2, 3, 4-tetrahydro-quinazoline or 2, 4-dioxo-1, 2, 3, 4-tetrahydroquinazoline ring at the 4-position were prepared and tested for antihypertensive activity. Among the compounds tested, 1-[2-hydroxy-2-(3, 4-methylenedioxyphenyl)ethyl]-4-(2, 4-dioxo-1, 2, 3, 4-tetrahydro-3-quinazolinyl)piperidine (20) and 1-[2-(4-chlorophenyl)-2-hydroxyethyl]-4-(2-oxo-1, 2, 3, 4-tetrahydro-3-quinazolinylmethyl)piperidine (30) produced relatively strong hypotension in the spontaneously hypertensive rat model.
一系列以2-氧代-1, 2, 3, 4-四氢喹唑啉或2, 4-二氧代-1, 2, 3, 4-四氢喹唑啉环在4位的哌啶衍生物被合成并测试了其抗高血压活性。在测试的化合物中,1-[2-羟基-2-(3, 4-亚甲基二氧基苯基)乙基]-4-(2, 4-二氧代-1, 2, 3, 4-四氢-3-喹唑啉基)哌啶(20)和1-[2-(4-氯苯基)-2-羟基乙基]-4-(2-氧代-1, 2, 3, 4-四氢-3-喹唑啉基甲基)哌啶(30)在自发性高血压大鼠模型中产生了相对较强的降压效果。