1,721,077 research outputs found
Versatility of the pyridazine system: Chemistry and biology
No full textIn accordance with the title of my lecture, I am going to briefly illustrate our researches on pyridazine derivatives active in different biological areas
Unexpected behaviour of the oxidizing agent sodium m-nitrobenzene sulfonate: synthesis of a new class of 5-hydroxy(1)benzopyrano4,3-cpyridazin-3(2H)ones
No full textSynthesis of a new series of 2,7-diazaspiro(3,5)nonan-1-ones and study of their cholinergic properties
No full textNon peptidic ligands at the opioid receptor like-1 (ORL-1)
No full textOpioid receptor like-1 (ORL-1) has recently been indicated as a potentially useful target for the treatment of a number of central disorders and several other diseases. This review deals with non peptidic ligands at the ORL-1 receptor, focusing on their structural and binding properties. Agonism or antagonism evidenced from functional experiments is also commented. For some compounds, possible therapeutic applications are considered
Synthesis of a new series of N-substituted-3(1-alkyl/aryl-4-piperidyl)azetidin-2-ones as possible muscarinic agents
No full textA new series of N-substituted-3-[1-alkyl(aryl)-4-piperidyl]azetidin-2- ones 2a-j structurally related to the previously reported 2,7- diazaspiro[3,5]nonan-1-ones 1 have been synthesized and tested for their activity as muscarinic agents, both in vitro and in vivo. Preliminary pharmacological results showed that compounds 2 are devoid of significant cholinergic properties
Hydroxymethylation of 2-hydroxypropiophenones in aqueous medium. Synthesis of 3-hydroxymethyl-3-methyl-4-chromanones and their conversion to 3-methyl-4-chromanone-3-acetic acids
No full text
Synthesis and pharmacological evaluation of a new class of 2-oxo-8-azaspiro(4,5)decan-1-ones as analogues of the muscarinic agonist RS-86
No full textA new series of 8-substituted-2-oxo-8-azapsiro (4,5)decan-1-ones has been synthesized and compounds tested for their cholinergic properties in comparison with the muscarinic agonist RS-86. Preliminary in vitro and in vivo pharmacological data indicate that none of them is provided with significant cholinergic effects either at central or peripheral level. A possible explanation for the lack of activity is given on the basis of conformational studies
Conformationally constrained congeners of 6-aryl-5-methyl-4,5-dihydro-3(2H)-pyridazinones active on the cardiovascular system: conformational studies by molecular mechanics calculations and proton NMR spectroscopy
No full textUnsubstituted phenylpyridazinones 1a and 2a and their tricyclic analogues indenopyridazinone 3a, benzocinnolinone 4a, and benzocycloheptapyridazinone 5a were submitted to conformational analysis with Allinger's MM2(85) program in order to better define the relationship between the cardiovascular properties of some derivatives and their preferred conformations. Structures 1-4, giving rise to highly active compounds, were found to exist in a conformation showing a near-planar arrangement of the phenyl and the pyridazinone ring. On the contrary, 5, whose derivatives were inactive, shows two significantly populated conformations both markedly deviated from planarity. 1H NMR analysis of the tricyclic systems 3-5 was in full agreement with the molecular mechanics calculations
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