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[具有抗胃酸分泌和抗溃疡活性的化合物。V. 3,3,4a,6,7,11b-六氢-2H,5H-苯并[1,4]环庚[1,2-b][1,4]-恶嗪的衍生物及相关产物]

[Compounds with anti-gastric secretion and antiulcer activity. V. Derivatives of 3,3,4a,6,7,11b-hexahydro-2H,5H-benzo [1,4]cyclohep[1,2-b][1,4]-oxazine and related products].

作者信息

Bianchi M, Butti A, Pfeiffer U, Rossi S, Barzaghi F, Marcaria V, Nencioni A

出版信息

Farmaco Sci. 1986 Mar;41(3):229-56.

PMID:3709787
Abstract

A series of hexahydrobenzo[3,4]cyclohept[1,2-b][1,4]oxazines, with different substituents at the benzene and oxazine rings and nitrogen atom, was synthetized. The diastereomers and enantiomers of the unsubstituted compound and the related derivatives hexahydrobenzo[5,6] and exahydrobenzo[6,7]cyclohept[1,2-b][1,4]oxazine, hexahydro[1]benzoxepine and hexahydro[1]benzothiepin[5,4-b][1,4]oxazine, octahydrobenzo[3,4]cyclohept[1,2-b][1,4]diazine were also prepared. Some of these compounds inhibited at low doses gastric secretion in pylorus-ligated rats and antagonized ulcers in pylorus-ligated rats plus acetylsalicylic acid and in cold+restraint-stressed rats. When the most active compounds were tested on cats with Heidenhain pouch, they induced unwanted side effects that ruled out further development of these chemical series.

摘要

合成了一系列在苯环、恶嗪环和氮原子上具有不同取代基的六氢苯并[3,4]环庚[1,2 - b][1,4]恶嗪。还制备了未取代化合物及其相关衍生物六氢苯并[5,6]和六氢苯并[6,7]环庚[1,2 - b][1,4]恶嗪、六氢[1]苯并氧杂卓和六氢[1]苯并硫杂卓[5,4 - b][1,4]恶嗪、八氢苯并[3,4]环庚[1,2 - b][1,4]二嗪的非对映异构体和对映异构体。其中一些化合物在低剂量时可抑制幽门结扎大鼠的胃酸分泌,并拮抗幽门结扎大鼠加乙酰水杨酸以及冷应激和束缚应激大鼠的溃疡。当对具有海登海因小胃的猫测试最具活性的化合物时,它们产生了不良副作用,这排除了这些化学系列的进一步开发。

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