- Big catkin willow acids compounds and medical use
-
The invention discloses a AMPK agonist activity with salicylic acid compound and its preparation method and medical use, it is the structural formula of the formula (I) compound of formula, its pharmaceutically acceptable salt or prodrug or solvate. The structure of the invention of formula (I) compound of formula activated AMPK, therefore can be used for preparing the prevention or treatment of AMPK mediated diseases.
- -
-
-
- Novel salicylanilides from 4,5-dihalogenated salicylic acids: Synthesis, antimicrobial activity and cytotoxicity
-
Salicylanilides have proved their activity against tuberculosis (TB). One weak electron-withdrawing substituent is favored at the salicylic part, specially Cl or Br atoms at positions 4 or 5. On the other hand, the antimycobacterial activity of salicylanilides is negatively affected when a strong electron-withdrawing substituent ([sbnd]NO2) is present at the same positions. Herein we describe the synthesis and characterization of novel salicylanilides possessing two weak electron-withdrawing groups (halogen atoms) at their salicylic part and compare their antitubercular activity with their monohalogenated analogues. All dihalogenated derivatives proved to possess antitubercular activity at a very narrow micromolar range (MIC?=?1–4?μM), similar with their most active monohalogenated analogues. More importantly, the most active final molecules were further screened against multidrug resistant strains and found to inhibit their growth at the range of 0.5–4?μM.
- Paraskevopoulos, Georgios,Monteiro, Sara,Vosátka, Rudolf,Krátky, Martin,Navrátilová, Lucie,Trejtnar, Franti?ek,Stola?íková, Ji?ina,Vin?ová, Jarmila
-
p. 1524 - 1532
(2017/02/18)
-
- Structure activity relationship for derivatives of xipamide (4 chloro 5 sulfamoyl 2',6' salicyloxylidide)
-
The synthesis of various derivatives of 4 chlorosalicylic acid substituted in position 5 is described. The evaluation of their diuretic potency on the rat showed 4 chloro 5 sulfamoyl 2',6' salicyloxylidide (BE 1293, xipamide, 'Aquaphor') as the most effective. The normal urinary volume is increased 10 fold by an oral dose of 100 mg/kg body weight. All changes in the molecular structure of xipamide, even acetylation, the introduction of a second sulfamoyl group or the exchange of the sulfonic group for the carbonyl group lead to a decrease in activity.
- Liebenow,Leuschner
-
p. 240 - 244
(2007/10/09)
-