10324-43-3Relevant academic research and scientific papers
Palladium-promoted arylation of functionalised organolithium compounds via their zinc derivatives
Yus, Miguel,Gomis, Joaquin
, p. 1989 - 1995 (2002)
The reaction of different functionalised organolithium compounds 2, 5, 8, and 13 [easily prepared by DTBB-catalysed lithiation of isochromane (1), phthalane (4), 2,3-dihydrobenzofuran (7) and 1-chloro-3,3-diethoxypropane (12), respectively] with an equimo
C-ARYL GLYCOSIDE COMPOUNDS FOR THE TREATMENT OF DIABETES AND OBESITY
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Page/Page column 91, (2009/10/30)
This invention relates to a compound of generic formula (I): (I) as well as a pharmaceutically acceptable salt thereof, a tautomer, optical isomer or a mixture of optical isomers in any proportion, in particular a mixture of enantiomers, and particularly a racemate mixture, in particular for use thereof as a drug, notably in the treatment of diabetes.
Tricyclic alkylamides as melatonin receptor ligands with antagonist or inverse agonist activity
Lucini, Valeria,Pannacci, Marilou,Scaglione, Francesco,Fraschini, Franco,Rivara, Sivia,Mor, Marco,Bordi, Fabrizio,Plazzi, Pier Vincenzo,Spadoni, Gilberto,Bedini, Annalida,Piersanti, Giovanni,Diamantini, Giuseppe,Tarzia, Giorgio
, p. 4202 - 4212 (2007/10/03)
This work reports the design and synthesis of novel alkylamides, characterized by a dibenzo[a,d] cycloheptene nucleus, as melatonin (MLT) receptor ligands. The tricyclic scaffold was chosen on the basis of previous quantitative structure-activity studies on MT1 and MT2 antagonists, relating selective MT2 antagonism to the presence of an aromatic substituent out of the plane of the MLT indole ring. Some dibenzo seven-membered structures were thus selected because of the noncoplanar arrangement of their benzene rings, and an alkylamide chain was introduced to fit the requirements for MLT receptor binding, namely, dibenzocycloheptenes with an acylaminoalkyl side chain at position 10 and dibenzoazepines with this side chain originating from the nitrogen atom bridging the two phenyl rings. Binding affinity at human cloned MT1 and MT2 receptors was measured by 2[125I] iodomelatonin displacement assay and intrinsic activity by the GTPγS test. The majority of the compounds were characterized by higher affinity at the MT2 than at the MT 1 receptor and by very low intrinsic activity values, thus confirming the importance of the noncoplanar arrangement of the two aromatic rings for selective MT2 antagonism. Dibenzocycloheptenes generally displayed higher MT1 and MT2 affinity than dibenzoazepines. N-(8-Methoxy-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-10-ylmethyl)propionamide (4c) and -butyramide (4d) were the most selective MT2 receptor antagonists of the series, with MT2 receptor affinity comparable to that of melatonin and as such among the highest reported in the literature for MLT receptor antagonists. The acetamide derivative 4b produced a noticeable reduction of GTPγS binding at MT2 receptor, thus being among the few inverse agonists described.
A Novel Series of Selective, Non-Peptide Inhibitors of Angiotensin II Binding to the AT2 Site
VanAtten, Mary K.,Ensinger, Carol L.,Chiu, Andrew T.,McCall, Dale E.,Nguyen, Tam T.,et al.
, p. 3985 - 3992 (2007/10/02)
The availability of peptide and non-peptide Ang II receptor antagonists has permitted the study of Ang II receptor heterogeneity.It is now widely recognized that there are at least two distinct Ang II receptor subtypes.AT1 receptors are selective in their recognition of agents such as losartan, DuP 532,L-158,809,SKF108566, and similar non-peptides.To date, all of the well-known actions of Ang II in mammals are blocked by the AT1 selective antagonists such as losartan and are thus designated as being mediated by the AT1 receptor.Although there have been reports of functional activity mediated through AT2 sites, the pharmacological role for the AT2 receptor has not yet been elucidated.Herein, we report the chemistry and SAR on a novel series of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids which have selective affinity for AT2 receptors.The most potent of which (19) has an IC50 of 30 nM for the AT2 receptor in the rat adrenal radioligand binding assay.
