- A new sequential intramolecular cyclization based on the boekelheide rearrangement
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Pyrrolidines and piperidines were synthesized from (aminoalkyl)pyridine N-oxides with a general and quite efficient method developed by using di-tert-butylsilyl bis(trifluoromethanesulfonate) as a new promoter for a Boekelheide-type reaction. The use of a
- Massaro, Assunta,Mordini, Alessandro,Mingardi, Anna,Klein, Jens,Andreotti, Daniele
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experimental part
p. 271 - 279
(2011/02/28)
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- Identification of 4-(1H-Imidazol-4(5)-ylmethyl)pyridine (Immethridine) as a Novel, Potent, and Highly Selective Histamine H3 Receptor Agonist
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In this study, the piperidine ring of immepip and its analogues was replaced by a rigid heterocyclic pyridine ring. Many compounds in the series exhibit high affinity and agonist activity at the human histamine H3 receptor. Particularly, the 4-
- Kitbunnadaj, Ruengwit,Zuiderveld, Obbe P.,Christophe, Bernard,Hulscher, Saskia,Menge, Wiro M. P. B.,Gelens, Edith,Snip, Erwin,Bakker, Remko A.,Celanire, Sylvain,Gillard, Michel,Talaga, Patrice,Timmerman, Henk,Leurs, Rob
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p. 2414 - 2417
(2007/10/03)
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- Arylpiperazines and their use as metalloproteinase inhibiting agents (MMP)
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Arylpiperazines of formula (I) useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.
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Page/Page column 17
(2010/02/06)
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- Synthesis and Structure-Activity Relationships of Conformationally Constrained Histamine H3 Receptor Agonists
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Immepip, a conformationally constrained analogue of the histamine congener imbutamine, shows high affinity and functional activity on the human H 3 receptor. Using histamine and its homologues as prototypes, other rigid analogues containing eit
- Kitbunnadaj, Ruengwit,Zuiderveld, Obbe P.,De Esch, Iwan J. P.,Vollinga, Roeland C.,Bakker, Remko,Lutz, Martin,Spek, Anthony L.,Cavoy, Emile,Deltent, Marie-France,Menge, Wiro M. P. B.,Timmerman, Henk,Leurs, Rob
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p. 5445 - 5457
(2007/10/03)
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- Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists
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A series of heterocyclic 2-(3,5-dimethylphenyl)tryptamine derivatives was prepared and evaluated on a rat gonadotropin releasing hormone receptor assay. The carbon tether length and heterocyclic ring attached to the amino group of 2-(3,5-dimethylphenyl)tr
- Lin, Peter,Parikh, Mamta,Lo, Jane-Ling,Yang, Yi Tien,Cheng, Kang,Smith, Roy G,Fisher, Michael H,Wyvratt, Matthew J,Goulet, Mark T
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p. 1077 - 1080
(2007/10/03)
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- PHARMACOLOGICALLY ACTIVE TRIAZINONES
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The compounds are substituted 1,2,4-triazin-5-ones which are histamine H 2-antagonists. Two specific compounds of the present invention are 3-2-(5-methyl-4-imidazolylmethylthio)ethylamino!-6-(3-methoxybenzyl)-1,2, 4-tr iazin-5-one and 3-2-(5-methyl-4-imidazolylmethylthio)ethylamino!-6-(3-pyridylmethyl)-1,2,4-tr iazin-5-one.
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