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1.
Bioorg Med Chem Lett ; 23(6): 1760-2, 2013 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-23403081

RESUMO

A series of novel indole-imidazole derivatives have been prepared and evaluated in vitro on the aromatase inhibitory activities. The results suggested that proton or a small electron-withdrawing group at para-position of the phenyl ring would enhance the inhibitory activities and any bulky group should be avoided in order to keep a relative small volume for this kind of molecules.


Assuntos
Inibidores da Aromatase/síntese química , Aromatase/química , Desenho de Fármacos , Imidazóis/química , Indóis/química , Aromatase/metabolismo , Inibidores da Aromatase/química , Inibidores da Aromatase/metabolismo , Cristalografia por Raios X , Imidazóis/síntese química , Imidazóis/metabolismo , Conformação Molecular , Ligação Proteica , Relação Estrutura-Atividade
2.
Acta Crystallogr Sect E Struct Rep Online ; 68(Pt 4): o1081, 2012 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-22589945

RESUMO

In the title compound, C(19)H(14)F(3)N(3), the dihedral angles between the mean planes of the indole ring and the 4-CF(3)-phenyl and imidazole rings are 54.95 (4) and 61.36 (7)°, respectively.

3.
Journal of Preventive Medicine ; (12): 973-976, 2016.
Artigo em Chinês | WPRIM | ID: wpr-792544

RESUMO

Objective To explore the association between type 2 diabetes mellitus (T2DM)combined with non -alcoholic fatty liver disease (NAFLD)and serum adiponectin (APN)and its clinical significance.Methods A total of 76 patients who were initially diagnosed with T2DM or had been diagnosed with T2DM for less than three years and admitted to the endocrine department and its outpatient clinic of the Affiliated Hospital of Medical School of Ningbo University from August 2011 to July 2013 were selected as the subjects,and were assigned to group A or B,each consisting of 38 patients,based on the presence or absence of associated NAFLD.Another 30 healthy subjects receiving physical examination were assigned to the control group (NC group).The indicators including body mass index (BMI),blood lipids,blood glucose,liver function,insulin resistance index (HOMA -IR)and serum APN,were measured and compared among the groups. Results In group A ,the indicators including BMI,triglyceride (TG),total cholesterol (TC),low density lipoprotein -cholesterol (LDL -C),alanine aminotransferase (ALT),fasting insulin (FINS)and HOMA -IR were significantly higher than those in group B and NC group,and the APN level was significantly lower than that in group B and NC group (P <0.05).Pearson correlation analysis indicated that APN was negatively correlated with BMI,TG,high density lipoprotein -cholesterol(HDL -C),and HOMA -IR,and positively correlated with TC,LDL -C and ALT(P <0.05).Multiple linear regression analysis suggested that HDL -C and HOMA -IR was the independent influencing factors for APN (P <0.05).Conclusion Severe insulin resistance and glucose and lipid metabolic disorders are present in T2DM patients combined with NAFLD,and adiponectin level is of vital significance for the development and progression of NAFLD.

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