Condensed thienopyrimidines. I. Synthesis and gastric antisecretory activity of 2,3-dihydro-5H-oxazolothienopyrimidin-5-one derivatives.
作者:Mitsuo SUGIYAMA、Toshiaki SAKAMOTO、Keiichi TABATA、Kazuo ENDO、Keiichi ITO、Mitsuko KOBAYASHI、Hiroshi FUKUMI
DOI:10.1248/cpb.37.2091
日期:——
A practical preparation of various 2, 3-dihydro-5H-oxazolo[3, 2-a]thieno[3, 2-d]-, [3, 4-d]-, and [2, 3-d]pyrimidin-5-one derivatives was developed starting from the corresponding aminothiopheneesters in two steps, and their chloro-substituted derivatives were prepared. These compounds were evaluated for gastric antisecretory activity in pylorus-ligated rats, compared to the anti-ulcer standard, cimetidine, and their structure-activity relationships are discussed.
一种实用的方法被开发用于合成多种2, 3-二氢-5H-噁唑并噻吩的[3, 2-a]、[3, 4-d]和[2, 3-d]嘧啶-5-酮衍生物,该过程从相应的氨基噻吩酯出发,仅需两步,并且其氯取代衍生物也被合成。这些化合物在幽门结扎大鼠中评估了其抗胃分泌活性,并与抗溃疡标准药物西咪替丁进行了比较,同时讨论了它们的结构-活性关系。