- Discovery of novel 3-benzylquinazolin-4(3H)-ones as potent vasodilative agents
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In the present study, a series of 3-benzylquinazolin-4(3H)-ones were synthesized and characterized. Their vasodilative effects were evaluated by wire myograph on isolated rat mesenteric arterial ring induced contraction with 60 mM KCl. The SAR of target compounds was discussed preliminarily. Among these compounds, 2a and 2c displayed potent vasodilatation action and could compete significantly the rat mesenteric arterial rings induced contraction with phenylephrine. Compounds 2a and 2c were further tested for their antihypertensive effects in SHR by oral administration. The results indicated that 2a and 2c could reduce significantly both diastolic and systolic blood pressure. Moreover, 2c displayed antihypertensive effect in a dose dependent manner, and could maintain the effects for 6 h at a dosage of 4.0 mg/kg. These findings suggest that the title compounds are novel vasodilative agents, representing a novel series of promising antihypertensive agents.
- Zuo, Sai-Jie,Li, Sen,Yu, Rui-Hong,Zheng, Guo-Xun,Cao, Yong-Xiao,Zhang, San-Qi
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p. 5597 - 5601
(2015/01/08)
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- N-SUBSTITUTED PIPERIDINE DERIVATIVES AS SEROTONIN RECEPTOR AGENTS
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Disclosed herein are substantially pure forms of the compounds of Formula (I), (II), (III), (IV) and (V), or a pharmaceutically acceptable salt, prodrug, hydrate, solvate, polymorph, stereoisomer or ester thereof. Also disclosed are methods of inhibiting an activity of a serotonin receptor, methods inhibiting an activation of a serotonin receptor, and methods of alleviating or treating various disease conditions and side effects.
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Page/Page column 75; 76
(2010/11/04)
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- Anthranilic acid derivatives as inhibitors of the cGMP-phosphodiesterase
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Compounds of formula (I) STR1where R 1 is hydrogen; R 2 is nitro, cyano or halo(lower)alkyl; R 3 is phenyl substituted with one or more substituents selected from halogen, cyano and lower alkoxy; A is a lower alkylene group; R 4 is a group CR 6 R 7 R 8 wherein R 6 and R 7 form, together with the carbon atom to which they are attached a cycloalkyl group optionally substituted with hydroxy, lower alkoxy or a lower alkanoylamino; and R 8 is hydrogen; its prodrug and a salt thereof.
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- A Facile Total Synthesis of (+/-)-Cherylline via an Aziridinium Intermediate
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The 4-aryl-1,2,3,4-tetrahydroisoquinoline alkaloid, (+/-)-cherylline (1), has been synthesised by a ring-opening reaction of the quaternary aziridinium salt, followed by a cyclisation of the quinone methide.
- Kametani, Tetsuji,Higashiyama, Kimio,Honda, Toshio,Otomasu, Hirotaka
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p. 2935 - 2938
(2007/10/02)
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