- Discovery of substituted phenyl urea derivatives as novel long-acting β2-adrenoreceptor agonists
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The synthesis of diverse functionalized ureas in a semi-parallel fashion is described, as well as their β1/β2-adrenergic activities and the corresponding structure-activity relationship (SAR). We have focused on lipophilicity and duration of action, and we have discovered a strong correlation in this series of molecules. A quantitative structure-activity relationship (QSAR) analysis will be presented that quantifies this relationship.
- Pérez, Daniel,Crespo, Maribel,Solé, Laia,Prat, Maria,Carcasona, Carla,Calama, Elena,Otal, Raquel,Gavaldá, Amadeu,Gómez-Angelats, Mireia,Miralpeix, Montserrat,Puig, Carles
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p. 1545 - 1548
(2011/04/16)
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- Derivatives of 4-(2-amino-1-hydroxyethyl)phenol as agonists of the b2 adrenergic receptor
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The present invention provides a compound of formula (I): wherein: R1 is a group selected from -CH2OH,-NHCOH and R2 is a hydrogen atom; or R1 together with R2 form the group -NHC(O)CH=CH-, wherein the nitrogen atom is bound to the carbon atom in the phenyl ring holding R1 and the carbon atom is bound to the carbon atom in the phenyl ring holding R2, R3a and R3b are independently selected from the group consisting of hydrogen atoms and C1-4 alkyl groups n is an integer selected from 0 to 6, R4 is selected from the group consisting of an optionally substituted monocyclic or polycyclic C3-10 cycloalkyl group, an optionally substituted monocyclic C5-10 aryl group and, a methyl group which is substituted with one or more substituents selected from C5-10 aryl and C5-10 aryloxy groups, wherein the monocyclic or polycyclic C3-10 cycloalkyl and the monocyclic C5-10 aryl groups independently are optionally substituted with one or more substituents selected from halogen atoms, C1-4 alkyl, C1-4 alkoxy, C5-10 aryl and C5-10 aryloxy groups, or a pharmaceutically-acceptable salt or solvate or stereoisomer thereof.
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Page/Page column 24
(2009/09/26)
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