- Synthesis and investigation of anti-inflammatory activity of novel nitric oxide donating hybrid drugs
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A small library of nitric oxide donating groups, 4-acetamidophenyl-2-[{2- (nitrooxy)ethyl}(phenyl) amino]benzoate (5a-e) possessing a variety of substituents (-H, -NO2, -CH3, -acetamidophenyl, -SO 2NH2) attached to the fourth position of phenyl ring were synthesized and evaluated for anti-inflammatory, analgesic and ulcerogenic potential. Structure-activity relationship data showed that the 2-phenylaminobenzoic acid skeleton is required for selective COX-2 inhibition. Among all compounds 4-acetamidophenyl-2-[{2-(nitrooxy)ethyl}(phenyl)amino] benzoate (5a) has shown potent anti-inflammatory activity while 4-acetamidophenyl-2-[{4-{(4-acetamidophenoxy)carbonyl} phenyl}{2-(nitrooxy) ethyl}amino]benzoate (5d) has shown potent analgesic activity compared to standard drug diclofenac.
- Chandak, Shailesh L.,Bansode, Amol S.,Murumkar, Prashant R.,Shinde, Monika G.,Bothara, Kailash G.
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p. 3510 - 3517
(2013/07/11)
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- Intramolecular N-aza-amidoalkylation in association with Witkop-Winterfeldt oxidation as the key step to synthesize Luotonin-A analogues
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An expedient four-step approach for the synthesis of a short library of original analogues of the Topo-I Luotonin-A inhibitor, substituted at their C8- and N15-positions, was investigated. This consists of Rutaecarpines formation, their Witkop-Winterfeldt oxidation followed ultimately with functional adjustment of the pyrroloquinolone intermediates. In the first step of these investigations, Rutaecarpines including the Topo-I poison Evodiamine were obtained via the new tandem N-acylation/aza-amidoalkylation using a nitrogen atom as an internal nucleophile with or without association with a decarboxylation.
- Pin, Frédéric,Comesse, Sébastien,Da?ch, Adam
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experimental part
p. 5564 - 5571
(2011/08/09)
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- NEW DS DNA BINDING FLUORESCENT DYES
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The present invention is directed to a fluorescent dye comprising a benzothiazolium moiety and a pyrimidinium moiety connected by a mono-methine bridge, characterized in that (i) the 2-position of the pyrimidine carries a substituent which starts with a C
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Page/Page column 17; Sheet 1
(2008/12/05)
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- SUBSTITUTED CYCLOHEXYL-1,4-DIAMINE DERIVATIVES WITH A CHAIN EXTENSION
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The invention relates to substituted cyclohexyl-1,4-diamine derivatives, to a method for their production, to medicaments containing said compounds and to the use of substituted cyclohexyl-1,4-diamine derivatives for producing medicaments.
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Page/Page column 25
(2008/06/13)
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