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1.
Acta Crystallogr Sect E Struct Rep Online ; 66(Pt 9): i65, 2010 Aug 11.
Artigo em Inglês | MEDLINE | ID: mdl-21588472

RESUMO

The quaternary title compound, caesium chromium(III) hepta-thio-diphosphate(V), CsCrP(2)S(7), has been synthesized using the reactive halide flux method. It is isotypic with other AMP(2)S(7) (A = alkali metal; M = Cr, V or In) structures and consists of two-dimensional (∞) (2)[CrP(2)S(7)](-) layers extending parallel to (001) which are separated from each other by Cs(+) ions (symmetry 2). The layer is built up from slightly distorted octa-hedral [CrS(6)] units (symmetry 2) and bent [P(2)S(7)] units consisting of two corner-sharing [PS(4)] tetra-hedra. The [CrS(6)] octa-hedra share two edges and two corners with the [PS(4)] tetra-hedra. There are only van der Waals inter-actions present between the layers. The Cs(+) ions are located in this van der Waals gap and stabilize the structure through weak ionic inter-actions. The classical charge balance of the title compound can be expressed as [Cs(+)][Cr(3+)][P(5+)](2)[S(2-)](7.).

2.
J Med Chem ; 51(22): 7216-33, 2008 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-18954042

RESUMO

Since the CB1 cannabinoid receptor antagonist 1 (SR141716, rimonabant) was previously reported to modulate food intake, CB1 antagonism has been considered as a new therapeutic target for the treatment of obesity. In the present study, biarylpyrazole analogues based on a pyrazole core coupled with 1,3,4-oxadiazole were synthesized and tested for CB1 receptor binding affinity. Thorough SAR studies to optimize pyrazole substituents as well as 1,3,4-oxadiazole ring led to several novel CB1 antagonists with IC(50) approximately 1 nM for the CB1 receptor binding. Among these analogues, we identified 2-(4-((1H-1,2,4-triazol-1-yl)methyl)-5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-1H-pyrazol-3-yl)-5-(1-(trifluoromethyl)cyclopropyl)-1,3,4-oxadiazole 43c as a promising precandidate for the development as an antiobesity agent.


Assuntos
Obesidade/tratamento farmacológico , Oxidiazóis/farmacologia , Pirazóis/farmacologia , Receptor CB1 de Canabinoide/antagonistas & inibidores , Administração Oral , Animais , Disponibilidade Biológica , Simulação por Computador , Cristalografia por Raios X , Relação Dose-Resposta a Droga , Humanos , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Modelos Químicos , Modelos Moleculares , Estrutura Molecular , Oxidiazóis/síntese química , Oxidiazóis/química , Pirazóis/síntese química , Pirazóis/química , Ratos , Ratos Sprague-Dawley , Receptor CB2 de Canabinoide/antagonistas & inibidores , Estereoisomerismo , Relação Estrutura-Atividade
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