- Synthesis of Conformationally Locked and C-Linked Analogues of Imidazole-Based Ketene Dithioacetal Fungicides
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First examples with the unknown tricyclic 4,8 b -dihydro-3 aH -indeno[1,2- d ][1,3]dithiole ring system have been prepared. Also, imidazoles linked in ring position 5 to a ketene dithioacetal and 1,3-dithiane derivatives with an exocyclic cyano- and imidazole-substituted C-C double bond are completely new. All these compounds are either conformationally locked, C-linked or six-ring analogues of the antifungal agent luliconazole. Synthesis and fungicidal activity of these sterol biosynthesis inhibitors are reported.
- Gagnepain, Julien,Jeanmart, Stephane,Bonvalot, Damien,Jacob, Olivier,Lamberth, Clemens
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- Selective bromination of 4-chloro-1-indanone and synthesis of (4-chloro-2, 3-dihydro-1H-indene-2-yl)methanamine
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The synthesis of 4-chloro-1-indanone in four steps from 2-chlorobenzaldehyde was investigated. Bromination of this compound under various conditions occurred in the cyclopentanone ring, producing mono- and dibromo derivatives. Cyanation of 2-bromo-4-chlor
- Jasouri,Khalafy,Badali,Piltan
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- Synthesis and bioactivity of substituted indan-1-ylideneaminoguanidine derivatives
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In our efforts to discover more potent and lasting NHE1 inhibitors, we designed and synthesized a series of substituted indan-1-ylidene aminoguanidine derivatives (5). NHE1 inhibitory activity of twenty-one compounds 5 was evaluated in a rat platelet swelling assay. It is found that most of the tested compounds possess NHE1 inhibitory effects. 2-(5-methoxybenzimidazol-2-ylthio)-5-chloro-2,3-dihydroinden-1-ylidene aminoguanidine hydrobromide (5m) proved to be sixty-nine times more potent than cariporide. Furthermore, when tested in vivo, compound 5m also displayed superior cardioprotective effects against SD rat myocardial ischemic-reperfusion injury over those of cariporide.
- Zhang, Rui,Dong, Jin,Xu, Yun-gen,Hua, Wei-yi,Wen, Na,You, Qi-dong
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experimental part
p. 3771 - 3776
(2009/12/04)
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- 8-Methylureido-4,5-dihydro-4-oxo-10H-imidazo[1,2-a]indeno[1,2-e]pyrazines : Highly potent in vivo AMPA antagonists
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A novel series of readily water soluble 8-methylureido-4,5-dihydro-4-oxo-10H-imidazo[1,2-a]indeno[1,2-e]pyrazines were synthesized. The -10-yl acetic acid ((+)-3) and -10-carboxylidene (4) derivatives exhibit potent affinities (IC50 = 4 and 19 nM, respectively) and antagonist properties (IC50 = 2 and 3 nM, respectively) at the ionotropic AMPA receptor. These compounds also display anticonvulsant properties against both electrically and sound-induced convulsions in mice after ip, sc and iv administration with ED50 values between 0.9 and 11 mg/kg, thus suggesting adequate brain penetration. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Mignani, Serge,Bohme, Georg Andrees,Boireau, Alain,Cheve, Michel,Damour, Dominique,Debono, Marc-Williams,Genevois-Borella, Arielle,Imperato, Assunta,Jimonet, Patrick,Pratt, Jeremy,Randle, John C.R.,Ribeill, Yves,Vuilhorgne, Marc,Stutzmann, Jean-Marie
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p. 591 - 596
(2007/10/03)
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- Derivatives of 5H, 10H-imidazo[1, 2-a]indeno[1,2-e]pyrazin-4-one, preparation thereof and medicaments containing them
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Compounds having the formula (I) wherein R and R 1, similar or different, represent a hydrogen or halogen atom or a radical alkyl, alkoxy, amino, acylamino, phenylureido, --N CH--N(R 2)R 3, nitro, imidazolyl, phenyl, SO 3 H or cyano; R 2 and R 3 which may
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